Journal articles: 'In vitro antimycobacterial evaluation'

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Al, Matarneh, Catalina Ciobanu, Ionel Mangalagiu, and Ramona Danac. "Design, synthesis and antimycobacterial evaluation of some new azaheterocycles with the 4,7-phenanthroline skeleton. Part VI." Journal of the Serbian Chemical Society 81, no. 2 (2016): 133–40. http://dx.doi.org/10.2298/jsc150514084a.

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A feasible study concerning the synthesis, structure and in vitro antimycobacterial evaluation of new 4,7-phenanthroline derivatives is reported. The preparation is straight and efficient, involving an N-alkylation reaction of 4,7-phenanthroline. The structure of the new compounds have been proved by elemental and spectral (IR, 1H and 13C NMR) analysis. The in vitro antimycobacterial evaluation of five synthesized compounds was investigated against Mycobacterium tuberculosis H37Rv under aerobic conditions. A certain influence of substituents from the para position of the benzoyl moiety was observed, the 4,7-phenanthrolin-4-ium salt substituted with (p)chloro-benzoyl showing the most pronounced antimycobacterial activity.

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Kumar Baba, N. H., D. Ashok, Boddu Ananda Rao, Sarasija Madderla, and N. Y. S. Murthy. "Microwave-assisted synthesis and biological evaluation of thiazole-substituted dibenzofurans." Heterocyclic Communications 24, no. 3 (June 27, 2018): 171–76. http://dx.doi.org/10.1515/hc-2017-0247.

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AbstractNew thiazole-substituted dibenzofurans 7a–j were synthesized from dibenzofuran derivatives 5a–b and substituted thiosemicarbazones 6a–h under conventional and microwave irradiation conditions. The structures of all products were established on the basis of analytical and spectral data. The synthesized compounds were evaluated for their in vitro antibacterial activity against Gram-positive and Gram-negative strains. Compounds 7b, 7d and 7h are active against Bacillus subtilis (+ve), and compound 7i displays good activity against Pseudomonas aeruginosa (-ve) strain. Compounds 7a–j were also evaluated for their in vitro antimycobacterial activity, and compound 7b shows antimycobacterial activity against Mycobacterium bovis strain.

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Kumar, Deepak, Garima Khare, Beena Beena, Saqib Kidwai, Anil K. Tyagi, Ramandeep Singh, and Diwan S. Rawat. "Novel isoniazid–amidoether derivatives: synthesis, characterization and antimycobacterial activity evaluation." MedChemComm 6, no. 1 (2015): 131–37. http://dx.doi.org/10.1039/c4md00288a.

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Tosun, F., Ç. Akyüz Kızılay, B. Şener, and M. Vural. "The Evaluation of Plants from Turkey forin Vitro. Antimycobacterial Activity." Pharmaceutical Biology 43, no. 1 (January 2005): 58–63. http://dx.doi.org/10.1080/13880200590903372.

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Baranyai, Zsuzsa, Martin Krátký, Rudolf Vosátka, Eleonóra Szabó, Zsuzsanna Senoner, Sándor Dávid, Jiřina Stolaříková, Jarmila Vinšová, and Szilvia Bősze. "In vitro biological evaluation of new antimycobacterial salicylanilide-tuftsin conjugates." European Journal of Medicinal Chemistry 133 (June 2017): 152–73. http://dx.doi.org/10.1016/j.ejmech.2017.03.047.

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Bouz, Ghada, Sarah Bouz, Ondřej Janďourek, Klára Konečná, Pavel Bárta, Jarmila Vinšová, Martin Doležal, and Jan Zitko. "Synthesis, Biological Evaluation, and In Silico Modeling of N-Substituted Quinoxaline-2-Carboxamides." Pharmaceuticals 14, no. 8 (August 4, 2021): 768. http://dx.doi.org/10.3390/ph14080768.

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Despite the established treatment regimens, tuberculosis remains an alarming threat to public health according to WHO. Novel agents are needed to overcome the increasing rate of resistance and perhaps achieve eradication. As part of our long-term research on pyrazine derived compounds, we prepared a series of their ortho fused derivatives, N-phenyl- and N-benzyl quinoxaline-2-carboxamides, and evaluated their in vitro antimycobacterial activity. In vitro activity against Mycobacterium tuberculosis H37Ra (represented by minimum inhibitory concentration, MIC) ranged between 3.91–500 µg/mL, with most compounds having moderate to good activities (MIC < 15.625 µg/mL). The majority of the active compounds belonged to the N-benzyl group. In addition to antimycobacterial activity assessment, final compounds were screened for their in vitro cytotoxicity. N-(naphthalen-1-ylmethyl)quinoxaline-2-carboxamide (compound 29) was identified as a potential antineoplastic agent with selective cytotoxicity against hepatic (HepG2), ovarian (SK-OV-3), and prostate (PC-3) cancer cells lines. Molecular docking showed that human DNA topoisomerase and vascular endothelial growth factor receptor could be potential targets for 29.

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Opletalová, Veronika, Milan Pour, Jiří Kuneš, Vladimír Buchta, Luís Silva, Katarína Kráľová, Marta Chlupáčová, Dana Meltrová, Milan Peterka, and Martina Posledníková. "Synthesis and Biological Evaluation of (E)-3-(Nitrophenyl)-1-(pyrazin-2-yl)prop-2-en-1-ones." Collection of Czechoslovak Chemical Communications 71, no. 1 (2006): 44–58. http://dx.doi.org/10.1135/cccc20060044.

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The title (E)-(3-nitrophenyl)-1-(pyrazin-2-yl)prop-2-en-1-ones were prepared by the Claisen- Schmidt condensation of acetylpyrazines and 2-nitro-, 3-nitro- and 4-nitrobenzaldehyde in pyridine using diethylamine as the catalyst. The compounds were bioassayed for in vitro antifungal, antimycobacterial and photosynthesis-inhibiting activity. The high potency of (E)-1-(5-tert-butylpyrazin-2-yl)-3-(4-nitrophenyl)prop-2-en-1-one againstMycobacterium tuberculosis(MIC 0.78 μg/ml) and moderate activities of several compounds againstTrichophyton mentagrophytesandCandidaspp. do not support the assumption that phenolic groups are essential for antimycobacterial and antifungal activity of chalcones and their analogues. In fact, the nitro-substituted compounds were superior to the previously described hydroxylated congeners with antimycobacterial activity (MIC ≥ 12.5 μg/ml). The compounds also reduced chlorophyll content in green algaChlorella vulgaris, and some of them inhibited photosynthetic electron transport in spinach chloroplasts as well. The photosynthesis-inhibiting activity of nitro derivatives was lower than that of the corresponding hydroxylated analogues.

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Ambrożkiewicz, Weronika, Marta Kučerová-Chlupáčová, Ondřej Janďourek, Klára Konečná, Pavla Paterová, Pavel Bárta, Jarmila Vinšová, Martin Doležal, and Jan Zitko. "5-Alkylamino-N-phenylpyrazine-2-carboxamides: Design, Preparation, and Antimycobacterial Evaluation." Molecules 25, no. 7 (March 28, 2020): 1561. http://dx.doi.org/10.3390/molecules25071561.

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According to the World Health Organization, tuberculosis is still in the top ten causes of death from a single infectious agent, killing more than 1.7 million people worldwide each year. The rising resistance developed by Mycobacterium tuberculosis against currently used antituberculars is an imperative to develop new compounds with potential antimycobacterial activity. As a part of our continuous research on structural derivatives of the first-line antitubercular pyrazinamide, we have designed, prepared, and assessed the in vitro whole cell growth inhibition activity of forty-two novel 5-alkylamino-N-phenylpyrazine-2-carboxamides with various length of the alkylamino chain (propylamino to octylamino) and various simple substituents on the benzene ring. Final compounds were tested against Mycobacterium tuberculosis H37Ra and four other mycobacterial strains (M. aurum, M. smegmatis, M. kansasii, M. avium) in a modified Microplate Alamar Blue Assay. We identified several candidate molecules with micromolar MIC against M. tuberculosis H37Ra and low in vitro cytotoxicity in HepG2 cell line, for example, N-(4-hydroxyphenyl)-5-(pentylamino)pyrazine-2-carboxamide (3c, MIC = 3.91 µg/mL or 13.02 µM, SI > 38) and 5-(heptylamino)-N-(p-tolyl)pyrazine-2-carboxamide (4e, MIC = 0.78 µg/mL or 2.39 µM, SI > 20). In a complementary screening, we evaluated the in vitro activity against bacterial and fungal strains of clinical importance. We observed no antibacterial activity and sporadic antifungal activity against the Candida genus.

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Bouz, Ghada, Lucia Semelková, Ondřej Janďourek, Klára Konečná, Pavla Paterová, Lucie Navrátilová, Vladimír Kubíček, Jiří Kuneš, Martin Doležal, and Jan Zitko. "Derivatives of 3-Aminopyrazine-2-carboxamides: Synthesis, Antimicrobial Evaluation, and in Vitro Cytotoxicity." Molecules 24, no. 7 (March 28, 2019): 1212. http://dx.doi.org/10.3390/molecules24071212.

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We report the design, synthesis, and in vitro antimicrobial activity of a series of N-substituted 3-aminopyrazine-2-carboxamides with free amino groups in position 3 on the pyrazine ring. Based on various substituents on the carboxamidic moiety, the series is subdivided into benzyl, alkyl, and phenyl derivatives. The three-dimensional structures of the title compounds were predicted using energy minimization and low mode molecular dynamics under AMBER10:EHT forcefield. Compounds were evaluated for antimycobacterial, antibacterial, and antifungal activities in vitro. The most active compound against Mycobacterium tuberculosis H37Rv (Mtb) was 3-amino-N-(2,4-dimethoxyphenyl)pyrazine-2-carboxamide (17, MIC = 12.5 µg/mL, 46 µM). Antimycobacterial activity against Mtb and M. kansasii along with antibacterial activity increased among the alkyl derivatives with increasing the length of carbon side chain. Antibacterial activity was observed for phenyl and alkyl derivatives, but not for benzyl derivatives. Antifungal activity was observed in all structural subtypes, mainly against Trichophyton interdigitale and Candida albicans. The four most active compounds (compounds 10, 16, 17, 20) were evaluated for their in vitro cytotoxicity in HepG2 cancer cell line; only compound 20 was found to exert some level of cytotoxicity. Compounds belonging to the current series were compared to previously published, structurally related compounds in terms of antimicrobial activity to draw structure activity relationships conclusions.

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Webster, Duncan, Timothy D. G. Lee, Jill Moore, Tracy Manning, Dennis Kunimoto, Darren LeBlanc, John A. Johnson, and Christopher A. Gray. "Antimycobacterial screening of traditional medicinal plants using the microplate resazurin assay." Canadian Journal of Microbiology 56, no. 6 (June 2010): 487–94. http://dx.doi.org/10.1139/w10-035.

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Multidrug-resistant Mycobacterium tuberculosis strains have rapidly become a global health concern. North American First Nations communities have used traditional medicines for generations to treat many pulmonary infections. In this study, we evaluated the antimycobacterial activity of 5 medicinal plants traditionally used as general therapeutics for pulmonary illnesses and specifically as treatments for tuberculosis. Aqueous extracts of Aralia nudicaulis , Symplocarpus foetidus , Heracleum maximum , Juniperus communis, and Acorus calamus were screened for antimycobacterial activity against Bacillus Calmette–Guérin, Mycobacterium avium, and M. tuberculosis H37Ra using the colorimetric microplate resazurin assay. Extracts of Acorus calamus and H. maximum root demonstrated significant antimycobacterial activity comparable to that of the rifampin control (2 µg/mL). Evaluation of the cytotoxicity of these 2 extracts using the MTT assay also showed that the extracts were less toxic to 3 human cell lines than was the DMSO positive control. This study demonstrates that aqueous extracts of the roots of H. maximum and Acorus calamus possess strong in vitro antimycobacterial activity, validates traditional knowledge, and provides potential for the development of urgently needed novel antituberculous therapeutics.

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Kampmann, Beate, Gwen N. Tena, Shumikazi Mzazi, Brian Eley, Douglas B. Young, and Michael Levin. "Novel Human In Vitro System for Evaluating Antimycobacterial Vaccines." Infection and Immunity 72, no. 11 (November 2004): 6401–7. http://dx.doi.org/10.1128/iai.72.11.6401-6407.2004.

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ABSTRACT Major research efforts are directed towards the development of a better antimycobacterial vaccine. But progress in the field of tuberculosis vaccine development has been hampered by the lack of human in vitro models to assess vaccine immunogenicity and efficacy. New candidate vaccines will have to be evaluated against the existing Mycobacterium bovis BCG “gold standard.” It is therefore important to understand the type of immune responses elicited by BCG vaccination to enable comparisons with potential new candidates. We used a novel human in vitro whole-blood model, which measures immune responses to mycobacteria by use of reporter gene-tagged BCG (BCG lux), to study immune responses to BCG vaccination in 50 neonates in a setting in Cape Town, Republic of South Africa, where tuberculosis is endemic. BCG vaccination significantly reduced growth of BCG lux in whole blood (prevaccination median growth ratio [GR], 9.6; range, 1.3 to 24; postvaccination median GR, 3.9; range, 0.6 to 12.2 [P < 0.0001]). Growth of BCG lux was better restricted in vaccinated infants than in unvaccinated age-matched controls (n = 4). BCG vaccination induced significantly higher gamma interferon production in response to BCG lux (P < 0.0001) and to purified protein derivative (P = 0.0001). No significant changes in either growth of BCG lux or cytokine production occurred in an adult control group (n = 6) over the study period. The whole-blood luminescence model detects changes in cellular immune responses to mycobacteria induced by BCG vaccination. It is therefore a useful new tool in studying the immunogenicity of newly developed vaccine candidates prior to large field trials assessing efficacy.

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12

Zitko, Jan, Alžběta Mindlová, Ondřej Valášek, Ondřej Jand’ourek, Pavla Paterová, Jiří Janoušek, Klára Konečná, and Martin Doležal. "Design, Synthesis and Evaluation of N-pyrazinylbenzamides as Potential Antimycobacterial Agents." Molecules 23, no. 9 (September 18, 2018): 2390. http://dx.doi.org/10.3390/molecules23092390.

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Three series of N-(pyrazin-2-yl)benzamides were designed as retro-amide analogues of previously published N-phenylpyrazine-2-carboxamides with in vitro antimycobacterial activity. The synthesized retro-amides were evaluated for in vitro growth inhibiting activity against Mycobacterium tuberculosis H37Rv (Mtb), three non-tuberculous mycobacterial strains (M. avium, M. kansasii, M. smegmatis) and selected bacterial and fungal strains of clinical importance. Regarding activity against Mtb, most N-pyrazinylbenzamides (retro-amides) possessed lower or no activity compared to the corresponding N-phenylpyrazine-2-carboxamides with the same substitution pattern. However, the active retro-amides tended to have lower HepG2 cytotoxicity and better selectivity. Derivatives with 5-chloro substitution on the pyrazine ring were generally more active compared to their 6-cloro positional isomers or non-chlorinated analogues. The best antimycobacterial activity against Mtb was found in N-(5-chloropyrazin-2-yl)benzamides with short alkyl (2h: R2 = Me; 2i: R2 = Et) in position 4 of the benzene ring (MIC = 6.25 and 3.13 µg/mL, respectively, with SI > 10). N-(5-Chloropyrazin-2-ylbenzamides with hydroxy substitution (2b: R2 = 2-OH; 2d: R2 = 4-OH) on the benzene ring or their acetylated synthetic precursors possessed the broadest spectrum of activity, being active in all three groups of mycobacterial, bacterial and fungal strains. The substantial differences in in silico calculated properties (hydrogen-bond pattern analysis, molecular electrostatic potential, HOMO and LUMO) can justify the differences in biological activities between N-pyrazinylbenzamides and N-phenylpyrazine-2-carboxamides.

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Sardari, Soroush, Isabel Portugal, Abeer ALKafri, Danesh Moradi, and Ghazaleh Ghavami. "Fragment-Based De Novo Design of Antimycobacterial Agents and In Vitro Potency Evaluation." Combinatorial Chemistry & High Throughput Screening 19, no. 3 (March 22, 2016): 238–45. http://dx.doi.org/10.2174/1386207319666160219113649.

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Abou El Seoud, Kamilia A. E. H., Michael C. Bibby, Nagwa Shoeib, and Colin W. Wright. "Evaluation of Some Egyptian Plant Species for in vitro Antimycobacterial and Cytotoxic Activities." Pharmaceutical Biology 41, no. 6 (January 2003): 463–65. http://dx.doi.org/10.1076/phbi.41.6.463.17831.

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KARADAĞ, Ayşe Esra, Ayşegül ÇAŞKURLU, and Fatma TOSUN. "In Vitro Anti-Helicobacter Pylori and Antimycobacterial Activity Evaluation Of Selected Plants From Turkey." Journal of Anatolian Environmental and Animal Sciences 5, no. 2 (June 30, 2020): 231–35. http://dx.doi.org/10.35229/jaes.689341.

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Antoun, M. D., Z. Ramos, J. Vazques, I. Oquendo, G. R. Proctor, L. Gerena, and S. G. Franzblau. "Evaluation of the flora of Puerto Rico for in vitro antiplasmodial and antimycobacterial activities." Phytotherapy Research 15, no. 7 (2001): 638–42. http://dx.doi.org/10.1002/ptr.880.

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Madikizela, Balungile, Tamira Eckhardt, Richard Goddard, Adrian Richter, Anika Lins, Christoph Lehmann, Peter Imming, and Rüdiger W. Seidel. "Synthesis, structural characterization and antimycobacterial evaluation of several halogenated non-nitro benzothiazinones." Medicinal Chemistry Research 30, no. 8 (June 10, 2021): 1523–33. http://dx.doi.org/10.1007/s00044-021-02735-4.

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Abstract8-Nitro-1,3-benzothiazin-4-ones (BTZs), with BTZ043 and PBTZ169 as the most advanced compounds, represent a new class of potent antitubercular agents, which irreversibly inhibit decaprenylphosphoryl-β-d-ribose-2′-epimerase (DprE1), an enzyme crucial for cell wall synthesis in the pathogen Mycobacterium tuberculosis. Synthesis, structural characterization and in vitro testing against Mycobacterium aurum DSM 43999 and M. tuberculosis H37Rv of halogenated 2-(4-ethoxycarbonylpiperazin-1-yl)-1,3-benzothiazin-4-ones lacking a nitro group are reported. X-ray crystallography reveals that the structure of the BTZ scaffold can significantly deviate from planarity. In contrast to recent reports, the results of the present study indicate that further investigation of halogenated non-nitro BTZs for antitubercular activity is less than a promising approach.

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García-Davis, Sara, Karla Leal-López, Carmen A. Molina-Torres, Lucio Vera-Cabrera, Ana R. Díaz-Marrero, José J. Fernández, Pilar Carranza-Rosales, and Ezequiel Viveros-Valdez. "Antimycobacterial Activity of Laurinterol and Aplysin from Laurencia johnstonii." Marine Drugs 18, no. 6 (May 30, 2020): 287. http://dx.doi.org/10.3390/md18060287.

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Marine environments represent a great opportunity for the discovery of compounds with a wide spectrum of bioactive properties. Due to their large variety and functions derived from natural selection, marine natural products may allow the identification of novel drugs based not only on newly discovered bioactive metabolites but also on already known compounds not yet thoroughly investigated. Since drug resistance has caused an increase in infections by Mycobacterium tuberculosis and nontuberculous mycobacteria, the re-evaluation of known bioactive metabolites has been suggested as a good approach to addressing this problem. In this sense, this study presents an evaluation of the in vitro effect of laurinterol and aplysin, two brominated sesquiterpenes isolated from Laurencia johnstonii, against nine M. tuberculosis strains and six nontuberculous mycobacteria (NTM). Laurinterol exhibited good antimycobacterial activity, especially against nontuberculous mycobacteria, being remarkable its effect against Mycobacterium abscessus, with minimum inhibitory concentration (MIC) values lower than those of the reference drug imipenem. This study provides further evidence for the antimycobacterial activity of some sesquiterpenes from L. johnstonii, which can be considered interesting lead compounds for the discovery of novel molecules to treat NTM infections.

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A, Mann, O. Amupitan J, O. Oyewale A, I. Okogun J, Ibrahim K, Oladosu P, Lawson L, Olajide I, and Nnamdi A. "Evaluation of in vitro antimycobacterial activity of Nigerian plants used for treatment of respiratory diseases." African Journal of Biotechnology 7, no. 11 (June 3, 2008): 1630–36. http://dx.doi.org/10.5897/ajb08.438.

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Ngadino, Setiawan, Koerniasari, Ernawati, and S. A. Sudjarwo. "Evaluation of antimycobacterial activity of Curcuma xanthorrhiza ethanolic extract against Mycobacterium tuberculosis H37Rv in vitro." Veterinary World 11, no. 3 (March 2018): 368–72. http://dx.doi.org/10.14202/vetworld.2018.368-372.

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Battah, Basem, Giulia Chemi, Stefania Butini, Giuseppe Campiani, Simone Brogi, Giovanni Delogu, and Sandra Gemma. "A Repurposing Approach for Uncovering the Anti-Tubercular Activity of FDA-Approved Drugs with Potential Multi-Targeting Profiles." Molecules 24, no. 23 (November 29, 2019): 4373. http://dx.doi.org/10.3390/molecules24234373.

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Tuberculosis (TB) is one of the top 10 causes of death worldwide. This scenario is further complicated by the insurgence of multidrug-resistant (MDR) and extensively drug-resistant (XDR) TB. The identification of appropriate drugs with multi-target affinity profiles is considered to be a widely accepted strategy to overcome the rapid development of resistance. The aim of this study was to discover Food and Drug Administration (FDA)-approved drugs possessing antimycobacterial activity, potentially coupled to an effective multi-target profile. An integrated screening platform was implemented based on computational procedures (high-throughput docking techniques on the target enzymes peptide deformylase and Zmp1) and in vitro phenotypic screening assays using two models to evaluate the activity of the selected drugs against Mycobacterium tuberculosis (Mtb), namely, growth of Mtb H37Rv and of two clinical isolates in axenic media, and infection of peripheral blood mononuclear cells with Mtb. Starting from over 3000 FDA-approved drugs, we selected 29 marketed drugs for submission to biological evaluation. Out of 29 drugs selected, 20 showed antimycobacterial activity. Further characterization suggested that five drugs possessed promising profiles for further studies. Following a repurposing strategy, by combining computational and biological efforts, we identified marketed drugs with relevant antimycobacterial profiles.

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Prashanthi Evangeline M, Prem Kumar P, and Bala Murugan K. "Cinnoline Derivatives as Antibacterial Agent and Antimycobacterial Agent: Synthesis, Microbial Evaluation and Molecular Docking Study." International Journal of Research in Pharmaceutical Sciences 11, no. 4 (November 17, 2020): 6675–84. http://dx.doi.org/10.26452/ijrps.v11i4.3588.

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Fourteen Novel cinnoline library compounds were designed, synthesized through a facile approach, and allowed for screening for anti-bacterial activity and anti-tubercular activity. The titled compounds were entirely synthesized by replacing alkyl groups, sulphonyl, halo groups in the 6th & 7th position of cinnoline moiety. The enlightenment of structure was done by FTIR HNMR along with elemental analysis and further docked for Structural activity. The newly synthesized Cinnoline Compounds were examined for their in vitro drug-sensitive M tuberculosis H37Hv strain. All the compounds have shown MIC between >100-12.5 μg /ml. In this investigation, we Evaluated all the compounds for Anti-bacterial activity. The main compounds were initially tested in vitro for Anti-bacterial activity against gram-positive and gram-negative bacteria by using the Disk plate method. The most active Compound 10 exhibited 12.5 μg /ml inhibitions against drug-sensitive M Tuberculosis H37Rv strain. Among all synthesized compounds CN-7 was found to be a Hit compound with MIC value 12.5 ug/ml Against E Coli.

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Wei, Zengquan, Jian Wang, Mingliang Liu, Sujie Li, Lanying Sun, Huiyuan Guo, Bin Wang, and Yu Lu. "Synthesis, in Vitro Antimycobacterial and Antibacterial Evaluation of IMB-070593 Derivatives Containing a Substituted Benzyloxime Moiety." Molecules 18, no. 4 (March 28, 2013): 3872–93. http://dx.doi.org/10.3390/molecules18043872.

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Song, Dan-Qing, and et al et al. "ChemInform Abstract: Synthesis, Structure-Activity Relationship and in vitro Antimycobacterial Evaluation of 13-n-Octylberberine Derivatives." ChemInform 43, no. 39 (August 30, 2012): no. http://dx.doi.org/10.1002/chin.201239210.

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Gobis, Katarzyna, Henryk Foks, Marcin Serocki, Ewa Augustynowicz-Kopeć, and Agnieszka Napiórkowska. "Synthesis and evaluation of in vitro antimycobacterial activity of novel 1H-benzo[d]imidazole derivatives and analogues." European Journal of Medicinal Chemistry 89 (January 2015): 13–20. http://dx.doi.org/10.1016/j.ejmech.2014.10.031.

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Polkam, Naveen, Parsharamulu Rayam, Jaya Shree Anireddy, Satyanarayana Yennam, Hasitha Shilpa Anantaraju, Sriram Dharmarajan, Yogeeswari Perumal, Sudha Sravanti Kotapalli, Ramesh Ummanni, and Sridhar Balasubramanian. "Synthesis, in vitro anticancer and antimycobacterial evaluation of new 5-(2,5-dimethoxyphenyl)-1,3,4-thiadiazole-2-amino derivatives." Bioorganic & Medicinal Chemistry Letters 25, no. 7 (April 2015): 1398–402. http://dx.doi.org/10.1016/j.bmcl.2015.02.052.

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REIS, Luis F. C. DOS, Cláudio D. CERDEIRA, Bruno F. DE PAULA, Jeferson J. da SILVA, Luiz F. L. COELHO, Marcelo A. SILVA, Vanessa B. B. MARQUES, Jorge K. CHAVASCO, and Geraldo ALVES-DA-SILVA. "CHEMICAL CHARACTERIZATION AND EVALUATION OF ANTIBACTERIAL, ANTIFUNGAL, ANTIMYCOBACTERIAL, AND CYTOTOXIC ACTIVITIES OF Talinum paniculatum." Revista do Instituto de Medicina Tropical de São Paulo 57, no. 5 (October 2015): 397–405. http://dx.doi.org/10.1590/s0036-46652015000500005.

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SUMMARY In this study, the bioactivity of Talinum paniculatum was evaluated, a plant widely used in folk medicine. The extract from the T. paniculatum leaves (LE) was obtained by percolation with ethanol-water and then subjecting it to liquid-liquid partitions, yielding hexane (HX), ethyl acetate (EtOAc), butanol (BuOH), and aqueous (Aq) fractions. Screening for antimicrobial activity of the LE and its fractions was evaluated in vitro through broth microdilution method, against thirteen pathogenic and non-pathogenic microorganisms, and the antimycobacterial activity was performed through agar diffusion assay. The cytotoxic concentrations (CC90) for LE, HX, and EtOAc were obtained on BHK-21 cells by using MTT reduction assay. The LE showed activity against Serratia marcescens and Staphylococcus aureus, with Minimum Inhibitory Concentration (MIC) values of 250 and 500 µg/mL, respectively. Furthermore, HX demonstrated outstanding activity against Micrococcus luteus and Candida albicans with a MIC of 31.2 µg/mL in both cases. The MIC for EtOAc also was 31.2 µg/mL against Escherichia coli. Conversely, BuOH and Aq were inactive against all tested microorganisms and LE proved inactive against Mycobacterium tuberculosisand Mycobacterium bovisas well. Campesterol, stigmasterol, and sitosterol were the proposed structures as main compounds present in the EF and HX/EtOAc fractions, evidenced by mass spectrometry. Therefore, LE, HX, and EtOAc from T. paniculatumshowed potential as possible sources of antimicrobial compounds, mainly HX, for presenting low toxicity on BHK-21 cells with excellent Selectivity Index (SI = CC90/MIC) of 17.72 against C. albicans.

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Bhat, Mashooq A., Mohamed A. Al-Omar, Ahmed M. Naglah, and Azmat Ali Khan. "Synthesis of Novel Sulfamethaoxazole 4-Thiazolidinone Hybrids and Their Biological Evaluation." Molecules 25, no. 16 (August 6, 2020): 3570. http://dx.doi.org/10.3390/molecules25163570.

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A search for potent antitubercular agents prompted us to design and synthesize sulfamethaoxazole incorporated 4-thiazolidinone hybrids (7a–l) by using a cyclocondensation reaction between 4-amino-N-(5-methylisoxazol-3-yl)benzenesulfonamide (4), aryl aldehyde (5a–l), and mercapto acetic acid (6) resulting in good to excellent yields. All the newly synthesized 4-thiazolidinone derivatives were screened for their in vitro antitubercular activity against M. Bovis BCG and M. tuberculosis H37Ra (MTB) strains. The compounds 7d, 7g, 7i, 7k, and 7l revealed promising antimycobacterial activity against M. Bovis and MTB strains with IC90 values in the range of 0.058–0.22 and 0.43–5.31 µg/mL, respectively. The most active compounds were also evaluated for their cytotoxicity against MCF-7, HCT 116, and A549 cell lines and were found to be non-cytotoxic. Moreover, the synthesized compounds were also analyzed for ADME (absorption, distribution, metabolism, and excretion) properties and showed potential as good oral drug candidates.

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Guillon, Jean, Robert C. Reynolds, Jean-Michel Leger, Marie-Aude Guie, Stephane Massip, Patrick Dallemagne, and Christian Jarry. "Synthesis and PreliminaryIn Vitro Evaluation of Antimycobacterial Activity of New Pyrrolo[1,2-a]quinoxaline-carboxylic Acid Hydrazide Derivatives." Journal of Enzyme Inhibition and Medicinal Chemistry 19, no. 6 (December 1, 2004): 489–95. http://dx.doi.org/10.1080/14756360412331280464.

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Kumar, Deepak, Beena, Garima Khare, Saqib Kidwai, Anil K. Tyagi, Ramandeep Singh, and Diwan S. Rawat. "Synthesis of novel 1,2,3-triazole derivatives of isoniazid and their in vitro and in vivo antimycobacterial activity evaluation." European Journal of Medicinal Chemistry 81 (June 2014): 301–13. http://dx.doi.org/10.1016/j.ejmech.2014.05.005.

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Giftson, Paul, Jerrine Joseph, Revathy Kalyanasundaram, V. Ramesh Kumar, and Wilson Aruni. "In vitro evaluation of the anti-mycobacterial properties of the extracts of Momordica Charantia." Research Journal of Biotechnology 16, no. 7 (June 25, 2021): 15–22. http://dx.doi.org/10.25303/167rjbt1521.

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Tuberculosis (TB) is a communicable disease and remains one of the top 10 causes of death worldwide. One fourth of the world population is infected with TB at a risk of developing disease. The increase in the incidence of drug resistant TB around the world urges the need to develop a new candidate to fight against the disease. Plants were considered as the rich source of bioactive components to be used as potential drugs. Medicinal plants are used in pure as well as crude materials for their medicinal properties. Our research aims in identifying the phyto-molecules which have anti- tuberculosis property. Four medicinal plants namely, Acalyphaciliata (Kuppaimeni), Solanumtrilobatum (Thuthuvalai), Momordicacharantia (Bitter Gourd) and Sennaauriculata (Avaram) were chosen to evaluate their antimicrobial activity focusing on anti-tubercular activity. The methanol extracts of the medicinal plants showed significant inhibitory activity against bacterial and fungal pathogens. Sennaauriculata methanol extracts showed activity against S. aureus, E. coli, P. aeruginosa and C. albicans. In the screening of antimycobacterial activity done by LRP assay, among the plant extracts tested, the hexane crude extracts of Momordicacharantia (Bitter Gourd) showed 82.2% and 81.03% of inhibition against M. tuberculosis H37Rv at 500µg/ml and 250µg/ml concentration respectively. Similarly, the methanol crude extracts of Momordicacharantia showed 87.14% and 63.55% of inhibition at 500µg/ml and 250µg/ml concentration respectively.

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Ibrahim, Tarek S., Ehab S. Taher, Ebtihal Samir, Azizah M. Malebari, Ahdab N. Khayyat, Mamdouh F. A. Mohamed, Riham M. Bokhtia, et al. "In Vitro Antimycobacterial Activity and Physicochemical Characterization of Diaryl Ether Triclosan Analogues as Potential InhA Reductase Inhibitors." Molecules 25, no. 14 (July 8, 2020): 3125. http://dx.doi.org/10.3390/molecules25143125.

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Two sets of diphenyl ether derivatives incorporating five-membered 1,3,4-oxadiazoles, and their open-chain aryl hydrazone analogs were synthesized in good yields. Most of the synthesized compounds showed promising in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv. Three diphenyl ether derivatives, namely hydrazide 3, oxadiazole 4 and naphthylarylidene 8g exhibited pronounced activity with minimum inhibitory concentrations (MICs) of 0.61, 0.86 and 0.99 μg/mL, respectively compared to triclosan (10 μg/mL) and isoniazid (INH) (0.2 μg/mL). Compounds 3, 4, and 8g showed the InhA reductase enzyme inhibition with higher IC50 values (3.28–4.23 µM) in comparison to triclosan (1.10 µM). Correlation between calculated physicochemical parameters and biological activity has been discussed which justifies a strong correlation with respect to the inhibition of InhA reductase enzyme. Molecular modeling and drug-likeness studies showed good agreement with the obtained biological evaluation. The structural and experimental information concerning these three InhA inhibitors will likely contribute to the lead optimization of new antibiotics for M. tuberculosis.

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K, Kalaiselvi, Mangayarkarasi V, Gomathi Ns, Balaji S, Shivshankar R. Mane, and Raja Shunmugam. "LUCIFERASE REPORTER MYCOBACTERIOPHAGES FOR EVALUATING NORBORNENE-BASED ANTITUBERCULOSIS DRUG SUSCEPTIBILITY TESTING ON MYCOBACTERIUM TUBERCULOSIS." Asian Journal of Pharmaceutical and Clinical Research 10, no. 9 (September 1, 2017): 406. http://dx.doi.org/10.22159/ajpcr.2017.v10i9.19660.

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Objective: In 2015, 9.6 million people around the world became sick with tuberculosis (TB) disease and 1.5 million TB-related deaths worldwide. Recent increasing incidence of multidrug-resistant (MDR; resistance to at least rifampicin (RIF) and isoniazid [INH]) and extensively drug-resistant (MDR resistance plus resistance to a fluoroquinolone and an aminoglycoside) makes TB a serious concern. Lot of research is needed to deal with this infectious disease for a better alternative in treatment or modification of these older TB drugs. The present study aimed at evaluating antimycobacterial activity of norbornene (NOR) derived INH copolymer with poly ethylene glycol (NOR- polyethylene glycol [PEG]-INH) a novel nanocarrier along with the anti-TB drug using luciferase reporter phages (LRPs).Methods: NOR derived INH accounts for 74% of INH, 24% of NOR, and 2% of PEG. H37Rv control strain, a sensitive, and a resistant strain of Mycobacterium TB (MTB) used in this study. The in vitro activity of the drug was evaluated using absolute concentration method. The resistant strain was evaluated using LRP assay to observe the minimum inhibitory concentration of the drug.Results: Reduction in light units was observed for the resistant strain exposed to plain INH and NOR-PEG-INH separately. 24% of reduction was observed in strains exposed to plain INH whereas 37% of reduction was observed in strains exposed to NOR-PEG-INH.Conclusion: NOR-based INH had better antimycobacterial activity compared to plain INH and RIF. Antimycobacterial activity of INH and RIF increases even with very low dosage with NOR conjugate.

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Avupati, Vasudeva Rao, Rajendra Prasad Yejella, Venkateswara Rao Parala, Kishore Naidu Killari, Venkata Madhava Reddy Papasani, Prasad Cheepurupalli, Venkateswara Rao Gavalapu, and Bhavani Boddeda. "Synthesis, characterization and in vitro biological evaluation of some novel 1,3,5-triazine–Schiff base conjugates as potential antimycobacterial agents." Bioorganic & Medicinal Chemistry Letters 23, no. 21 (November 2013): 5968–70. http://dx.doi.org/10.1016/j.bmcl.2013.08.063.

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Asfaw, Henok, Thomas Wetzlar, Maria Santos Martinez-Martinez, and Peter Imming. "An efficient synthetic route for preparation of antimycobacterial wollamides and evaluation of their in vitro and in vivo efficacy." Bioorganic & Medicinal Chemistry Letters 28, no. 17 (September 2018): 2899–905. http://dx.doi.org/10.1016/j.bmcl.2018.07.021.

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Sriram, Dharmarajan, Perumal Yogeeswari, Devambatla Ravi Kumar Vyas, Palaniappan Senthilkumar, Pritesh Bhat, and Madala Srividya. "5-Nitro-2-furoic acid hydrazones: Design, synthesis and in vitro antimycobacterial evaluation against log and starved phase cultures." Bioorganic & Medicinal Chemistry Letters 20, no. 15 (August 2010): 4313–16. http://dx.doi.org/10.1016/j.bmcl.2010.06.096.

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Shawar, R. M., D. J. Humble, J. M. Van Dalfsen, C. K. Stover, M. J. Hickey, S. Steele, L. A. Mitscher, and W. Baker. "Rapid screening of natural products for antimycobacterial activity by using luciferase-expressing strains of Mycobacterium bovis BCG and Mycobacterium intracellulare." Antimicrobial Agents and Chemotherapy 41, no. 3 (March 1997): 570–74. http://dx.doi.org/10.1128/aac.41.3.570.

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The object of this study was to investigate the ability of a rapid luciferase assay to detect antimycobacterial activity in plant extracts. Recombinant strains of Mycobacterium bovis BCG (rBCG) and Mycobacterium intracellulare expressing firefly luciferase were used as the test organisms. Assays were conducted in a 96-well minitube format under biosafety level 2 conditions. Control and test wells were sampled immediately after inoculation and after 3 (recombinant M. intracellulare) and 5 (rBCG) days of incubation to measure luminescence with a microplate luminometer, and the relative change in luminescence was calculated as a percentage of control values. As an alternative test method, Alamar blue was added after 12 days of incubation, and changes in color were read visually. A total of 480 extracts were tested. Sixteen extracts were active against rBCG, and of those, seven were also active against recombinant M. intracellulare. With activity defined as a relative change in luminescence of < or = 1% (i.e., > or = 99% inhibition) and a persistence of blue color after addition of Alamar blue, there was 99.0% agreement between the two methods. Our results suggest that the luciferase assay is rapid and accurate and has the potential to greatly accelerate the evaluation of antimycobacterial activity in plant extracts in vitro. With this method, it is possible to screen a large number of samples in a short period of time.

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Andreevskaya, SN, TG Smirnova, EN Antonov, LN Chernousova, SE Bogorodsky, EE Larionova, VK Popov, and A. Ergeshov. "New in vitro model to evaluate kinetics of antimycobacterial drug release from bioresorbable polymeric carriers." MicroRNA in ocular pathology, no. 2020(4) (August 2020): 10–15. http://dx.doi.org/10.24075/brsmu.2020.050.

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Sustained-release drugs against tuberculosis are a promising approach to therapy since they positively affect patient compliance with long regimens, especially when it comes to the multidrug-resistant form of the disease. Conventional UV-visible spectroscopy does not work well with multicomponential culture media used for growing M. tuberculosis. The aim of this study was to develop a method for evaluating the kinetics of anti-tuberculosis drug released from bioresorbable polymeric carriers suitable for screening a wide range of encapsulated prolonged-release drugs and identifying the best performing candidate. While studying the growth dynamics of the laboratory susceptible strain M. tuberculosis H37Rv in the presence of different levofloxacin concentrations (from 0.03 to 0.4 μg/ml), we developed a model, which is essentially a set of 2 parallel experiments evaluating the kinetics of drug release into the culture medium. The results of these 2 experiments conducted on 3 encapsulated forms of levofloxacin loaded onto bioresorbable polymeric PLGA carriers (particles sized 50 μm and 100 μm and the matrix) revealed that release kinetics of the drug largely depended on the type of polymeric carrier. The best encapsulation of the antibiotic and its gradual release into the culture medium was observed for the matrix. All experiments were run in 3 replicates. The obtained data were analyzed using descriptive statistics.

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Washington, J. A. "Functions and activities of the Area Committee on Microbiology of the National Committee for Clinical Laboratory Standards." Clinical Microbiology Reviews 4, no. 2 (April 1991): 150–55. http://dx.doi.org/10.1128/cmr.4.2.150.

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The Area Committee on Microbiology of the National Committee for Clinical Laboratory Standards has responsibility for the development of guidelines and standards in the field of clinical microbiology. Through the consensus process, representatives from government, industry, and professional societies have developed standards on antibacterial susceptibility testing (M2, M7, and M11), antimycobacterial susceptibility testing (M24), quality assurance on commercially prepared microbiological culture media (M22), evaluation of production lots of dehydrated Mueller-Hinton agar (M6), and preparation and testing of fetal bovine serum for use as cell culture growth supplement (M25) and guidelines on bactericidal tests (M26), protection of laboratory workers from infections transmitted by blood, body fluids, and tissue (M29), blood film examination for parasites (M15), and development of in vitro susceptibility testing criteria and quality control parameters (M23).

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Mital, Alka, Rohani Prasad Burman, Rajesh Gour, Sarbjit Singh Jhamb, and Manjinder Singh Gill. "Synthesis, ADME Evaluation, and In Vitro Antimycobacterial Studies of a Novel Series of 2-Thiazolylimino-5-Arylidene-4-Thiazolidinone Derivatives." Anti-Infective Agents 15, no. 1 (April 20, 2017): 38–44. http://dx.doi.org/10.2174/2211352514666160929142142.

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Klemens, S. P., C. A. Sharpe, and M. H. Cynamon. "Activity of pyrazinamide in a murine model against Mycobacterium tuberculosis isolates with various levels of in vitro susceptibility." Antimicrobial Agents and Chemotherapy 40, no. 1 (January 1996): 14–16. http://dx.doi.org/10.1128/aac.40.1.14.

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The activity of pyrazinamide (PZA) against eight isolates of Mycobacterium tuberculosis in a murine infection model was evaluated. M. tuberculosis isolates with various degrees of in vitro susceptibility to PZA (MIC range, 32 to > 2,048 micrograms/ml) were used. Four-week-old female mice were infected intravenously with approximately 10(7) viable M. tuberculosis organisms. PZA at 150 mg/kg of body weight was started 1 day postinfection and given 5 days/week for 4 weeks. Infected but untreated mice were compared with PZA-treated mice. Mice were sacrificed at the completion of the treatment period, and viable cell counts were determined from homogenates of spleens and right lungs. PZA had activity in the murine test system against M. tuberculosis isolates for which the MICs were < or = 256 micrograms/ml. However, there was an inconsistent correlation between the absolute MICs and the reductions in organ viable cell counts. Studies with drug-resistant M. tuberculosis isolates with an isogenic background would improve evaluation of drug efficacy in the murine test system. Further evaluation of antimycobacterial agents against monodrug-resistant isolates will provide data that will be useful for development of algorithms for treatment of infection with drug-resistant organisms.

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ABUBAKAR, AMINU, B. S. Aliyu, S. Abdulkadir, R. B. Umar, and A. K. Maigari. "QUALITATIVE PHYTOCHEMICAL EVALUATION AND IN VITRO INHIBITION OF Mycobacterium tuberculosis USING METHANOLIC EXTRACTS OF Calotropis procera and Garcinia kola." FUDMA JOURNAL OF SCIENCES 4, no. 3 (September 30, 2020): 523–30. http://dx.doi.org/10.33003/fjs-2020-0403-285.

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Extracts of herbal plant samples which include leaves and seeds of Calotropis procera and Garcinia kola respectively were investigated for phytochemical content and tested against clinical isolates of Mycobacterium tuberculosis (in-vitro). 95% methanolic extract of the plant samples were obtained by percolation. The anti-mycobacterial activity was determined using disc diffusion method; Anova single factor was statistically used for the analysis. The crude methanol extract of Calotropis procera leaf and Garcinia kola seed reveal a final weight of 8.1g and 19.1g, tannins and flavonoids were the phytochemical compounds found to be present in all the plant samples. Rifampicin antibiotic was used as control and the antimycobacterial activity for the plant sample shows that C. procera has the highest zone of inhibition followed by G. kola, the minimum inhibitory concentration ranging from 500-2000ug/ml. The M.I.C of 95% methanol extract in the order mention above are 500-2000ug/ml and 1000-2000ug/ml. The result support the local use of these plants in the treatment of tuberculosis and it is suggested that these plants may have therapeutic value in the treatment of Tuberculosis. However, further investigations should be focused toward isolating chemical constituent that are responsible for pharmacological activities and identifying the compound eliciting the activities observed in the plant samples

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Bvumbi, Mpelegeng Victoria, Chris van der Westhuyzen, Edwin M. Mmutlane, and Andile Ngwane. "Riminophenazine Derivatives as Potential Antituberculosis Agents: Synthesis, Biological, and Electrochemical Evaluations." Molecules 26, no. 14 (July 10, 2021): 4200. http://dx.doi.org/10.3390/molecules26144200.

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A series of novel riminophenazine derivatives, having ionizable alkyl substituents at N-5 and a variety of substituents on the C-3 imino nitrogen, at C-8 and on the pendant aryl group, have been designed and synthesized. Preliminary investigations into the relationship between lipophilicity, redox potential, and antimycobacterial activity were conducted, using the in vitro activity against Mycobacterium tuberculosis H37Rv, mammalian cytotoxicity, and the redox potential of the compounds determined by cyclic voltammetry as measures. Results revealed an activity “cliff” associated with C-8 substitution (10l and 10m) that, along with defined redox activity, point to a new class of riminophenazines as potential anti-tuberculosis agents having reasonable activity (MIC99 ~1 µM).

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Avupati, Vasudeva Rao, Rajendra Prasad Yejella, Venkateswara Rao Parala, Kishore Naidu Killari, Venkata Madhava Reddy Papasani, Prasad Cheepurupalli, Venkateswara Rao Gavalapu, and Bhavani Boddeda. "ChemInform Abstract: Synthesis, Characterization and in vitro Biological Evaluation of Some Novel 1,3,5-Triazine-Schiff Base Conjugates as Potential Antimycobacterial Agents." ChemInform 45, no. 13 (March 14, 2014): no. http://dx.doi.org/10.1002/chin.201413189.

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Newton, Sandra M., Clara Lau, Sudagar S. Gurcha, Gurdyal S. Besra, and Colin W. Wright. "The evaluation of forty-three plant species for in vitro antimycobacterial activities; isolation of active constituents from Psoralea corylifolia and Sanguinaria canadensis." Journal of Ethnopharmacology 79, no. 1 (February 2002): 57–67. http://dx.doi.org/10.1016/s0378-8741(01)00350-6.

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Dobrikov, Georgi M., Violeta Valcheva, Yana Nikolova, Iva Ugrinova, Evdokia Pasheva, and Vladimir Dimitrov. "Efficient synthesis of new (R)-2-amino-1-butanol derived ureas, thioureas and acylthioureas and in vitro evaluation of their antimycobacterial activity." European Journal of Medicinal Chemistry 63 (May 2013): 468–73. http://dx.doi.org/10.1016/j.ejmech.2013.02.034.

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Aguirre-Rentería, Saúl A., Juan J. J. Carrizales-Castillo, María del Rayo Camacho Corona, Eugenio Hernández-Fernández, Elvira Garza-González, Verónica M. Rivas-Galindo, Eder Arredondo-Espinoza, and Francisco G. Avalos-Alanís. "Synthesis and in vitro evaluation of antimycobacterial and cytotoxic activity of new α,β-unsaturated amide, oxazoline and oxazole derivatives from -serine." Bioorganic & Medicinal Chemistry Letters 30, no. 9 (May 2020): 127074. http://dx.doi.org/10.1016/j.bmcl.2020.127074.

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Fernandes, Cassia Cristina, Priscila Mileide de Andrade, Tainá Caroline Lucena dos Santos, Mariana Brentini Santiago, Antônio Eduardo Miller Crotti, Carlos Henrique Gomes Martins, Lizandra Guidi Magalhães, and Mayker Lazaro Dantas Miranda. "In vitro evaluation of anticaries, antimycobacterial, antileishmanial and cytotoxic activities of essential oils from Eremanthus erythropappus and of α-bisabolol, their major sesquiterpene." February 2020, no. 14(02):2020 (February 20, 2020): 236–43. http://dx.doi.org/10.21475/ajcs.20.14.02.p1876.

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Interest in researches into medicinal plants and therapeutic effects of essential oils (EOs) on humans has increased over the last few years. Eremanthus erythropappus, known as candeia, is a Brazilian aromatic herbaceous plant whose α-bisabolol-rich oil has been used in several cosmetic preparations. This paper reports in vitro anticaries, antimycobacterial, antileishmanial and cytotoxic activities of EOs from E. erythropappus leaves (EL-EO) and stalks (ES-EO), besides α-bisabolol, their main sesquiterpene. EL-EO and ES-EO were extracted by hydrodistillation and analyzed by GC-FID and GC-MS. α-Bisabolol, cis-α-bisabolene and β-bisabolene were identified as their major constituents. Antibacterial activity of EOs was evaluated against eight standard strains of pathogens from the American Type Culture Collection (ATCC) by determining minimum inhibitory concentrations (MICs) with the use of the microdilution method. Antibacterial activity was evaluated against Streptococcus mutans, S. mitis, S. sanguinis, S. sobrinus, S. salivarius, Mycobacterium tuberculosis, M. avium and M. kansasii. EL-EO, ES-EO and α-bisabolol exhibited high leishmanicidal activity against promastigote forms of Leishmania amazonensis; IC50 values were 9.22 µg/mL, 6.00 µg/mL and 3.12 µg/mL, respectively. The 50% cytotoxic concentrations (CC50) of EL-EO, ES-EO and α-bisabolol against mouse peritoneal macrophages were 24.65 µg/mL, 8.87 µg/mL and 1021.00 µg/mL, respectively. These results suggest that EOs from E. erythropappus seem to be very promising for the development of new bactericidal and leishmanicidal agents.

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Pierson, Elise, Marie Haufroid, Tannu Priya Gosain, Pankaj Chopra, Ramandeep Singh, and Johan Wouters. "Identification and Repurposing of Trisubstituted Harmine Derivatives as Novel Inhibitors of Mycobacterium tuberculosis Phosphoserine Phosphatase." Molecules 25, no. 2 (January 19, 2020): 415. http://dx.doi.org/10.3390/molecules25020415.

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Mycobacterium tuberculosis is still the deadliest bacterial pathogen worldwide and the increasing number of multidrug-resistant tuberculosis cases further complicates this global health issue. M. tuberculosis phosphoserine phosphatase SerB2 is a promising target for drug design. Besides being a key essential metabolic enzyme of the pathogen’s serine pathway, it appears to be involved in immune evasion mechanisms. In this work, a malachite green-based phosphatase assay has been used to screen 122 compounds from an internal chemolibrary. Trisubstituted harmine derivatives were found among the best hits that inhibited SerB2 activity. Synthesis of an original compound helped to discuss a brief structure activity relationship evaluation. Kinetics experiments showed that the most potent derivatives inhibit the phosphatase in a parabolic competitive fashion with apparent inhibition constants ( K i ) values in the micromolar range. Their interaction modes with the enzyme were investigated through induced fit docking experiments, leading to results consistent with the experimental data. Cellular assays showed that the selected compounds also inhibited M. tuberculosis growth in vitro. Those promising results may provide a basis for the development of new antimycobacterial agents targeting SerB2.

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Narender, Malothu, Bhandaru Jaswanth S., Kulandaivelu Umasankar, Jojula Malathi, Adidala Raghuram Reddy, K. R. Umadevi, A. V. N. Dusthackeer, Kaki Venkat Rao, and Akkinepally Raghuram R. "Synthesis, in vitro antimycobacterial evaluation and docking studies of some new 5,6,7,8-tetrahydropyrido[4′,3′:4,5]thieno[2,3- d ]pyrimidin-4(3 H )-one schiff bases." Bioorganic & Medicinal Chemistry Letters 26, no. 3 (February 2016): 836–40. http://dx.doi.org/10.1016/j.bmcl.2015.12.083.

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Journal articles on the topic 'In vitro antimycobacterial evaluation'

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