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Journal articles on the topic 'In vitro antitubercular activity'

Author: Grafiati

Published: 5 June 2025

Last updated: 1 August 2025

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1

Anjani, Solankee, and Tailor Riki. "An efficient synthesis of some new chalcone, acetyl pyrazoline and amino pyrimidine bearing 1,3,5- triazine nucleus as potential antimicrobial and antitubercular agent." Chemistry International 2, no. 4 (2016): 189–200. https://doi.org/10.5281/zenodo.1471239.

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In an attempt to find a new class of antimicrobial and antitubercular agent, a new series of chalcone, acetyl pyrazoline and amino pyrimidine bearing 1,3,5- triazine nucleus were synthesized with appropriate chemical reagent. Chalcones (D1-D5) were synthesized by the classical Claisen-Schmidt condensation of substituted ketone (C) with variously substituted aldehydes via conventional method. Now treatment of chalcones with hydrazine hydrate/glacial acetic acid and guanidine hydrochloride/Alkali afforded the corresponding acetyl pyrazoline (E1-E5) and amino pyrimidine (F1-F5) derivatives respec

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2

Sriram, Dharmarajan, Perumal Yogeeswari, Prathiba Dhakla, Palaniappan Senthilkumar, and Debjani Banerjee. "N-Hydroxythiosemicarbazones: Synthesis and in vitro antitubercular activity." Bioorganic & Medicinal Chemistry Letters 17, no. 7 (2007): 1888–91. http://dx.doi.org/10.1016/j.bmcl.2007.01.037.

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3

Filitis, L. N., T. V. Akalaeva, O. Yu Amel'kin, A. I. Bokanov, P. Yu Ivanov, and V. I. Shvedov. "Synthesis and in vitro antitubercular activity of alkylaminotetrahydrocarbazoles." Pharmaceutical Chemistry Journal 22, no. 10 (1988): 780–85. http://dx.doi.org/10.1007/bf00763273.

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4

Dube, Phelelisiwe S., Dylan Hart, Lesetja J. Legoabe, Audrey Jordaan, Digby F. Warner, and Richard M. Beteck. "Synthesis and In Vitro Antibacterial Evaluation of Mannich Base Nitrothiazole Derivatives." Molbank 2024, no. 1 (2024): M1793. http://dx.doi.org/10.3390/m1793.

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Nitrothiazole derivatives have been reported to exhibit activity against aerobic, anaerobic, and microaerophilic bacteria. This activity profile makes the nitrothiazole compound class an ideal lead source against Mycobacterium tuberculosis, which flourishes in varied environments with different oxygen concentrations. In this work, we investigated six nitrothiazole derivatives for antitubercular activity. The compounds exhibited potent activity, with compounds 9 and 10 possessing an equipotent MIC90 value of 0.24 µM. The compounds were investigated for cytotoxicity against HEK293 cells and hemo

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5

Gopi, Chandravadivelu, Magharla Dasaratha Dhanaraju, Konatham Pranusha, Thiyagarajan Deepan, AR Magesh, and Dhanaraju Kavitha. "Design, Synthesis, Characterization and Antitubercular Activity of Novel Benzimidazole Mannich Base Derivatives." Asian Journal of Chemistry 36, no. 4 (2024): 969–73. http://dx.doi.org/10.14233/ajchem.2024.31314.

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In present work, the newly synthesized benzimidazole Mannich base derivatives were design, synthesized and evaluated the in silico and in vitro antitubercular activity. These compounds were synthesized by condensation reaction between 1-(1H-benzo[d]imidazol-1-yl)ethanone and aliphatic/aromatic amines. The synthesized compound structures were identified by FTIR, 13C NMR, 1H NMR and mass spectroscopies. The results indicated that these derivatives have significant antitubercular activity against Mycobacterium tuberculosis (M.tb) cell wall enzyme enoyl acyl carrier protein reductase (InhA), EthR

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6

Akula, Ravi K., Shanthan R. Pamulaparthy, Pranay K. Koochana, and Dharmarajan Sriram. "Synthesis and In vitro Antibacterial, Antitubercular Studies of Novel Fluoroquinolones Analogs Containing 4-substituted Sec Amine." Current Bioactive Compounds 15, no. 6 (2020): 656–64. http://dx.doi.org/10.2174/1573407214666180529124816.

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Background: Tuberculosis is a contagious, air borne disease and second leading cause of death among infectious diseases worldwide. Fluoroquinolones are well-known antibacterial agents and they were recommended as second-line of antitubercular drugs. Method: A series of novel fluoroquinolone analogs 6-24 was effectively synthesized. An attempt was made by tagging the substituted pyrazole on to fluoroquinolones for the first time at C-7 position. The newly synthesized compounds were characterized by FTIR, 1HNMR, ESI-MS, HR-MS and elemental analysis. The in vitro antibacterial activity of all the

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7

More, Uttam A., Joshi S.D, and V. H. Kulkarni. "Antitubercular Activity of Pyrrole Schiff bases and Computational Study of M. Tuberculosis InhA." International Journal of Drug Design and Discovery 4, no. 4 (2025): 1163–73. https://doi.org/10.37285/ijddd.4.4.1.

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Pursuing our search program for new antitubercular drugs we decided to explore the potentiality of pyrrole moiety by molecular modeling and synthesizing novel pyrrole Schiff bases analogues of phthivazid. Enoyl-acyl carrier protein reductase catalyzes the last rate-limiting step in the elongation cycle of the fatty-acid biosynthesis pathway and has been validated as a potential antitubercular drug target in Mycobacterium tuberculosis. The development of new antitubercular therapies is important both to combat potential drug-resistant bio weapons and to address the broader societal problem of i

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8

Santoso, Mardi, Muhammad Riza Ghulam Fahmi, Yehezkiel Steven Kurniawan, et al. "Isoniazid-Isatin Hydrazone Derivatives: Synthesis, Antitubercular Activity and Molecular Docking Studies." Trends in Sciences 18, no. 21 (2021): 39. http://dx.doi.org/10.48048/tis.2021.39.

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This study examined the synthesis of isoniazid-isatin hydrazone derivatives 5-7, followed by an investigation on the in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv, and molecular docking. A yield of 81 - 92 % of these compounds was achieved, with structural characterization by spectroscopic methods (FTIR, NMR, HRMS). The in vitro antitubercular activity was evaluated against M. tuberculosis H37Rv, and the highest effect was observed in compound 7, with a minimum inhibitory concentration (MIC) of 0.017 mM, lower than rifampicin (MIC 0.048 mM), which served as the posi

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9

Patel, Parth P., Navin B. Patel, Manesh S. Tople, Vatsal M. Patel, and Dhanji P. Rajani. "Microwave-Assisted Synthesis of 2-(Arylidene)-1-thia-4-azaspiro[4.5]decan-3-ones and their Antibacterial, Antitubercular, and In Silico Screening." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 33, no. 03 (2023): 285. http://dx.doi.org/10.59467/ijhc.2023.33.285.

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2-(Arylidene)-1-thia-4-azaspiro[4.5]decan-3-ones (3a-e, 4a-e) were synthesized from the 1-thia-4-azaspiro[4.5] decan-3-one through Knoevenagel reaction using the microwave method. In vitro, antibacterial and antitubercular screening of synthetic derivatives 3a-e and 4a-e revealed that compounds 3a and 4b are considerably potent as antibacterial agents against Escherichia coli with MIC = 50 μg/mL and MIC = 50 μg/mL, respectively. Compounds 3e and 4e possessed very good antitubercular activity with MIC = 0.47 μg/mL and MIC = 0.43 μg/mL. The results of molecular docking analysis supported the res

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10

Triveni, S., C. Naresh Babu, E. Bhargav, and M. Vijaya Jyothi. "in silico Design, ADME Prediction, Molecular Docking, Synthesis of Novel Triazoles, Indazoles & Aminopyridines and in vitro Evaluation of Antitubercular Activity." Asian Journal of Chemistry 32, no. 11 (2020): 2713–21. http://dx.doi.org/10.14233/ajchem.2020.22790.

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To design and synthesize novel triazoles, indazoles and aminopyridines from various (thiophene-2-yl)prop-2-en-1-one derivatives as antitubercular leads by in silico and in vitro methods. in silco Drug design, ADME prediction and molecular docking studies were performed to assess drug likeliness and antitubercular potential of all 30 novel triazoles, indazoles and aminopyridines. in silico Drug design studies revealed that the synthetic routes applied were appropriate according to the calculations of Swiss-ADME that measure synthetic accessibility. Most of the synthesized compounds found to hav

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11

Godge, Rahul, and Rahul Kunkulol. "SYNTHESIS OF COUMARIN HETEROCYCLIC DERIVATIVES WITH IN-VITRO ANTITUBERCULER ACTIVITY." Journal of Drug Delivery and Therapeutics 8, no. 5 (2018): 217–23. http://dx.doi.org/10.22270/jddt.v8i5.1859.

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In last few decades, though significant progress has been made in the treatment and control strategies of tubercular infections by introducing new diagnostic and monitoring tools and combination therapy, it still continues to be severe problem. The need of study was only because of there are many drugs in market to treat infection but most of the drugs are showing resistance because of the same it is difficult to treat the infection. In this study we chosen coumarin nucleus for study. Thus with the aim of developing novel molecule with improved potency for treating Mycobacterium tuberculosis H

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12

van der Westhuyzen, Christiaan W., Richard K. Haynes, Jenny-Lee Panayides, Ian Wiid, and Christopher J. Parkinson. "Anti-Mycobacterial Peroxides: A New Class of Agents for Development Against Tuberculosis." Medicinal Chemistry 16, no. 3 (2020): 392–402. http://dx.doi.org/10.2174/1573406415666190430143535.

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Background: With few exceptions, existing tuberculosis drugs were developed many years ago and resistance profiles have emerged. This has created a need for new drugs with discrete modes of action. There is evidence that tuberculosis (like other bacteria) is susceptible to oxidative pressure and this has yet to be properly utilised as a therapeutic approach in a manner similar to that which has proven highly successful in malaria therapy. Objective: To develop an alternative approach to the incorporation of bacterial siderophores that results in the creation of antitubercular peroxidic leads f

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13

Reddy, Venkata M., Leo Einck, and Carol A. Nacy. "In Vitro Antimycobacterial Activities of Capuramycin Analogues." Antimicrobial Agents and Chemotherapy 52, no. 2 (2007): 719–21. http://dx.doi.org/10.1128/aac.01469-07.

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ABSTRACT Translocase I inhibitor compounds derived from capuramycin demonstrated rapid bactericidal activity against several different mycobacterial species. SQ641 was the most active of the compounds, with a MIC of 0.12 to 8 μg/ml, a postantibiotic effect of 55 h, and interesting synergistic effects with other antitubercular drugs.

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14

Mahajan, Aman, Laurent Kremer, Stefan Louw, Yann Guéradel, Kelly Chibale, and Christophe Biot. "Synthesis and in vitro antitubercular activity of ferrocene-based hydrazones." Bioorganic & Medicinal Chemistry Letters 21, no. 10 (2011): 2866–68. http://dx.doi.org/10.1016/j.bmcl.2011.03.082.

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15

Kancharla, Sampath Kumar, Saritha Birudaraju, Arani Pal, et al. "Synthesis and biological evaluation of isatin oxime ether-tethered aryl 1H-1,2,3-triazoles as inhibitors of Mycobacterium tuberculosis." New Journal of Chemistry 46, no. 6 (2022): 2863–74. http://dx.doi.org/10.1039/d1nj05171g.

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16

BASAK, SUSMITA, and K. ISHWAR BHAT. "Design, Synthesis, Evaluation of Antitubercular and Antioxidant Activity of Isoxazoline Derivatives Derived from Novel Chalcone Intermediates." Asian Journal of Chemistry 35, no. 11 (2023): 2782–88. http://dx.doi.org/10.14233/ajchem.2023.30580.

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Tuberculosis (TB), a bacterial infection caused by Mycobacterium tuberculosis (M-TB) is a fatal disease associated with a high degree of mortality. Present work involved synthesis of a series of novel isoxazoline derivatives (ISOA1-ISOA8) the new antitubercular agents using newly synthesized chalcones (CHL1-CHL8). This was done by subjecting the chalcones to a reaction with hydroxylamine hydrochloride in presence of acetic acid and sodium acetate. The structure of the synthesized compounds was elucidated by IR, 1H NMR and mass spectra. In silico studies of isoxazoline were performed for antitu

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17

Prajapati, Krupa, Vikas Desai, Riki Tailor, Bhadresh Sudani, Priyank Mistry, and Jignesh Pandya. "Molecular hybridization of pyridine-thiophene clubbed isoxazole heterocycle in a single entity: Synthesis, antimicrobial, antitubercular, molecular docking and ADMET analysis." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 34, no. 03 (2024): 345. http://dx.doi.org/10.59467/ijhc.2024.34.345.

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In the present study, 10 new hybrid pyridine-thiophene clubbed isoxazole derivatives (8a-j) were synthesized from the reaction of benzylideneacetophenones (7a-j) with hydroxylamine hydrochloride in alkaline medium. The synthesized compounds were tested for in vitro antimicrobial and antitubercular properties. Four promising new lead compounds such as 8c, 8d, 8f, and 8h endowed with excellent antimicrobial and antitubercular activity. In addition, the docking score for the most active compounds 8b, 8e, 8g, and 8h was found to be -8.6 to -8.8 kcal/mol demonstrating its favorable accommodation wi

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18

Papageorgiou, Andria, Angeliki-Sofia Foscolos, Ioannis P. Papanastasiou, et al. "Synthesis, biology, computational studies and in vitro controlled release of new isoniazid-based adamantane derivatives." Future Medicinal Chemistry 11, no. 21 (2019): 2779–802. http://dx.doi.org/10.4155/fmc-2019-0038.

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Aim: There is a necessity for new drugs to be more efficient than today's standard due to the emergence of drug-resistant strains of Mycobacterium tuberculosis (Mtb) Results/methodology: 12 new isoniazid-based adamantane derivatives were synthesized and tested for their antitubercular activity. The pharmacological test results and the aqueous dissolution profile of representative examples of the new molecules are in agreement with the computational results obtained from docking poses and molecular dynamics simulations on the tested compounds. Conclusion: Among their congeners, the adamantane i

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19

Kardile, Deepak P., and Mrunal K. Shirsat. "Synthesis and in vitro Evaluation of Dihydrobenzimidazole Thiopyranooxazinone Derivatives as a Potent Biological Agents." Asian Journal of Organic & Medicinal Chemistry 5, no. 2 (2020): 164–70. http://dx.doi.org/10.14233/ajomc.2020.ajomc-p251.

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In the present study, dihydrobenzimidazole thiopyranooxazinone derivatives were efficiently synthesized, which were further characterized and authenticated by means of TLC and different spectral analysis such as IR and 1H NMR. The synthesized compounds DPK2d2 to DPK2d8 were screened for their in vitro antimicrobial, antitubercular and anticancer activities. The results showed that the titled compounds DPK3d1, DPK3d2 and DPK3d4 exhibited potent antimicrobial activity, shows a broadspectrum activity against Bacillus subtilis, Escherichia coli (antibacterial) and Aspergillus niger (antifungal) as

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20

K., P. Suhasini, Christopher V., Rama Mohana Rao S., Praveen Kumar Ch., and L. N. Murthy Y. "Synthesis, characterisation and antitubercular screening of 5(4H)-oxazolone derivatives." Journal of Indian Chemical Society Vol. 92, Jun 2015 (2015): 951–55. https://doi.org/10.5281/zenodo.5674257.

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Department of Organic Chemistry, Andhra University, Visakhapatnam-530 003, Andhra Pradesh, India <em>E-mail</em> : suhasini.kl@gmail.com, murthyyln@gmail.com Bio-Organic Chemistry Division, Indian Institute of Integrative Medicine, Jammu-180 001, J & K, India In search of new antitubercular agents, a new series of 4-(substituted benzylidene)-2-<em>p</em>-tolyloxazol-5(<em>4H</em>)-ones (5a-h) has been designed, synthesized and subjected to evaluate their antitubercular activity for the first time against <em>Mycobacterium tuberculosis</em> H37Rv, in comparison with standard drugs Rifampici

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21

Cassano, Roberta, Sonia Trombino, Teresa Ferrarelli, et al. "Synthesis, characterization and in-vitro antitubercular activity of isoniazid-gelatin conjugate." Journal of Pharmacy and Pharmacology 64, no. 5 (2012): 712–18. http://dx.doi.org/10.1111/j.2042-7158.2012.01461.x.

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22

Suman, Ashok Kumar, Anu Anu, and Bhawani Singh. "Synthesis and in vitro evaluation of tetrazole containing 1,5-benzothiazepines as new anticancer, antitubercular, antibacterial, and antifungal agents." European Journal of Chemistry 15, no. 3 (2024): 245–53. http://dx.doi.org/10.5155/eurjchem.15.3.245-253.2569.

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Heterocyclic scaffolds have attracted great attention of organic chemists and medicinal chemists, also because of their wide range of synthetic applicability and broad spectrum of biological profile. Therefore, in the present research work, a series of tetrazole containing 1,5-benzothiazepines have been synthesized for evaluation of their biological activities to determine the potential therapeutic profile of these compounds across various medicinal domains. Of the synthesized compounds, five compounds (6f, 8e, 8f, 8g, and 8h) have been screened for anticancer, antitubercular, antibacterial, a

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23

Ambrożkiewicz, Weronika, Marta Kučerová-Chlupáčová, Ondřej Janďourek, et al. "5-Alkylamino-N-phenylpyrazine-2-carboxamides: Design, Preparation, and Antimycobacterial Evaluation." Molecules 25, no. 7 (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-alky

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Posinasetty, Bhargavi, Ashish Ashokkumar Jaiswal, Rajendra Prasad Yejjella, Hari Veluru, Kishore Bandarapalle, and Rajasekhar Komarla Kumarachari. "Oxacyanopyridine-Benzofuran Hybrids: Synthesis, in silico Toxicity Assessment, in vitro Antimicrobial Activity and Dual Target Docking Studies." Asian Journal of Chemistry 36, no. 3 (2024): 593–602. http://dx.doi.org/10.14233/ajchem.2024.31092.

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This study emphasizes the synthesis and characterization of a novel series of oxa cyano pyridine heterocyclic molecular hybrids (OCP 1-6), integrating pyridine and benzofuran motifs. Meticulously designed from 5-chlorosalicylaldehyde in a multistep process, the synthesized compounds were structurally confirmed through IR spectroscopy, 1H NMR spectroscopy, and mass spectrometry. Computational predictions highlighted diverse properties, including antitubercular and antibacterial attributes, bioactivity scores, toxicity profiles and potential molecular targets. In vitro assessments and Schrödinge

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25

Zandhaghighi, Mehdi, Farzin Hadizadeh, Saman Soleimanpour, et al. "In vitro bactericidal activities of two novel dihydropyridine derivatives against Mycobacterium tuberculosis." Journal of Infection in Developing Countries 11, no. 06 (2017): 453–58. http://dx.doi.org/10.3855/jidc.7966.

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Introduction: Introducing new and effective antitubercular agents is important in tuberculosis control programs. In this study, the in vitro antitubercular activity of two novel 1,4-dihydropyridine derivatives (F-27, Cl-33) were screened against a total of 113 different strains of Mycobacterium tuberculosis (77 susceptible and 36 resistant clinical isolates). Methodology: The in vitro activities of these compounds were evaluated based on the modified broth macro-dilution assay. Results: Compound F-27 showed more than 90% growth inhibition at the range of 2 to 8 μg/mL (minimum inhib

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Gordon, Sara, Johayra Simithy, Douglas C. Goodwin, and Angela I. Calderón. "Selective Mycobacterium tuberculosis Shikimate Kinase Inhibitors as Potential Antibacterials." Perspectives in Medicinal Chemistry 7 (January 2015): PMC.S13212. http://dx.doi.org/10.4137/pmc.s13212.

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Owing to the persistence of tuberculosis (TB) as well as the emergence of multidrug-resistant and extensively drug-resistant (XDR) forms of the disease, the development of new antitubercular drugs is crucial. Developing inhibitors of shikimate kinase (SK) in the shikimate pathway will provide a selective target for antitubercular agents. Many studies have used in silico technology to identify compounds that are anticipated to interact with and inhibit SK. To a much more limited extent, SK inhibition has been evaluated by in vitro methods with purified enzyme. Currently, there are no data on in

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27

Sultana, Shameem, and G. Shiva Kumar. "Synthesis, Antimicrobial and Antitubercular Activity of Novel Imidazole Carboxamides." Asian Journal of Chemistry 35, no. 5 (2023): 1276–82. http://dx.doi.org/10.14233/ajchem.2023.27823.

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A series of novel imidazole carboxamide derivatives (6a-j) were synthesized in moderate to good yields via the oxidative esterification of 1H-imidazole-4-cabaldehyde (1) with phenol (4) followed by the aminolysis of various substituted anilines (5a-j) in the presence of 1,3-bis(2,6-diisopropylphenyl)imidazol-2-ylidene (2) (IPr, 10 mol%) and TEMPO (3) in toluene. All the compounds were characterized by IR, 1H NMR, 13C NMR and mass spectral data. The synthesized compounds were assessed in vitro for their antimicrobial and antitubercular potential. Among the synthesized compounds 6a, 6f and 6g ha

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Navin, Patel, Patel Sarvil, Purohit Amit, et al. "Synthesis and biological evaluation of newer 1,3,4-oxadiazoles incorporated with benzothiazepine and benzodiazepine moieties." Zeitschrift für Naturforschung C 72, no. 3-4 (2017): 133–46. http://dx.doi.org/10.1515/znc-2016-0129.

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Abstract A series of thiazepines and diazepines having 1,3,4-oxadiazole moiety were synthesized, and they were analyzed for their in vitro antimicrobial activity against several bacteria (Staphylococcus aureus, Staphylococcus pyogenes, Escherichia coli, and Pseudomonas aeruginosa) and fungi (Candida albicans, Aspergillus niger, and Aspergillus Clavatus) and protozoa (Entamoeba histolytica, Giardia lamblia, Trypanosoma cruzi and Leishmania mexicana). Few of the selected compounds were tested for their antitubercular activity. However, it was noticed that the potency of final analogs against eac

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Prasad, Sakshith Raghavendra, Nayak Devappa Satyanarayan, Avarse Satish Kumar Shetty, and Basaiah Thippeswamy. "Synthesis, antimicrobial, and antitubercular evaluation of new Schiff bases with in silico ADMET and molecular docking studies." European Journal of Chemistry 13, no. 1 (2022): 109–16. http://dx.doi.org/10.5155/eurjchem.13.1.109-116.2216.

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Schiff bases are a proven moiety in antitubercular drug discovery and the antitubercular drug development. Drug discovery is a never-ending process due to evolving drug resistance by the bacteria, as a result, there is a need of developing new antitubercular drugs. In this continuous process of antitubercular drug discovery, new series of Schiff bases are synthesized using quinoline carbohydrazide upon coupling with different aldehydes in ethanolic media through multistep synthesis. These synthesized compounds were purified and characterized by different spectroscopic techniques. The molecules

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Panda, Krishna Chandra, Bera Venkata Varaha Ravi Kumar, Biswa Mohan Sahoo, Bimal Krishna Banik, and Abhishek Tiwari. "Microwave Irradiated Eco-friendly Synthesis of Pyrimidine Derivatives as Potential Antitubercular Agents." Asian Journal of Chemistry 34, no. 4 (2022): 907–11. http://dx.doi.org/10.14233/ajchem.2022.23644.

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The microwave irradiation method is applied for the efficient synthesis of pyrimidine derivatives. The synthetic protocol involves Knoevenagel condensation followed by Michael addition reaction and cyclization of equimolar quantities of aromatic aldehydes, ethyl cyanoacetate and guanidine in the presence of ethanolic NaOH solution to produce corresponding pyrimidine derivatives. The reaction mixture was allowed to reflux under microwave radiation at power level-2 for 7-12 min. The microwave heating technique offers a cleaner reaction with a shorter reaction time and improved product yield as c

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Patel, Pinkal H., and Nadim M. R. Chhipa. "Synthesis, computational docking, and biological evaluation of some new N-arylacetate nitroimidazole derivatives against Mycobacterium tuberculosis." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 35, no. 01 (2025): 165. https://doi.org/10.59467/ijhc.2025.35.165.

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This research aimed to design and synthesize innovative derivatives of 4-mono and 3,4-disubstituted aryl 4'-nitroimidazole acetates. The synthesis of these compounds involved a condensation reaction between 4-nitroimidazoles and 4-mono/3,4-disubstituted phenyl acetates. Their potential antitubercular properties were evaluated through in vitro and in silico methodologies. The results demonstrated potent anti-tubercular effects of these derivatives against Mycobacterium tuberculosis, particularly in the H37Rv strain, The observed activity is likely due to the role of the deazaflavin-dependent ni

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32

Posinasetty, Bhargavi, Rajendra Prasad Yejjella, Kishore Bandarapalle, Rajasekhar Komarla Kumarachari, Hari Veluru, and Chilamakuru Naresh Babu. "Benzofuran-Isoxazole Hybrids: Synthesis, Antimicrobial Activity and Dual Target Docking Studies." Asian Journal of Chemistry 36, no. 1 (2023): 125–34. http://dx.doi.org/10.14233/ajchem.2024.30779.

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In this study, five novel heterocyclic molecular hybrids (4a-e) were synthesized by combining benzofuran and isoxazole motifs. Thesecompounds were synthesized via a multistep process starting with 5-chlorosalicylaldehyde. The structures of the synthesized compounds were characterized by IR, 1H NMR and mass spectrometry. Computational tools were employed to predict properties, including antitubercular and antibacterial traits, drug-likeness, bioactivity scores, toxicity and potential molecular targets. In addition to these predictions, in vitro bioactivities were assessed and conducted Schrödin

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33

Almehmadi, Mazen, Abdualziz Alsharif, Mamdouh Allahyani, and Mohammad Asif. "Microwave-assisted synthesis and in vitro antimycobacterial evaluation of some new N-benzylidene-1H-benzo[d]imidazol-6-amine derivatives." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 34, no. 03 (2024): 363. http://dx.doi.org/10.59467/ijhc.2024.34.363.

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N-Benzylidene-1H-benzo[d]-imidazol-6-amines (2a-f) were synthesized by the reaction between 1H-benzo[d] imidazol-6-amine and substituted aromatic aldehydes in the presence of ethyl alcohol and glacial acetic acid using microwave irradiation technique. The structures of the compounds were determined using elemental analysis, infrared, 1HNMR, and MS spectrum data. The microplate alamar blue assay method was used to test the synthesized compounds for their in vitro antimycobacterial activity against strains of Mycobacterium tuberculosis H37RV strain. Among tested compounds, compound 2a with a min

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Dasan, Neethu, G. Babu, and Shiny George. "MOLECULAR DOCKING STUDIES AND SYNTHESIS OF 3, 4 - DISUBSTITUTED TRIAZOLES AS MYCOBACTERIUM TUBERCULOSIS ENOYL-ACP REDUCTASE AND CYP-51 INHIBITORS." International Journal of Pharmacy and Pharmaceutical Sciences 11, no. 1 (2019): 85. http://dx.doi.org/10.22159/ijpps.2019v11i1.29428.

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Objective: To design, synthesize and in vitro antitubercular, antifungal and antioxidant evaluation of some novel mercapto 1, 2, 4–triazole derivatives.Methods: New derivatives were designed by using various software like ACD Lab chemsketch, molinspiration and autodock. Designed molecules are obeying Lipinski’s rule of five and having highest binding score was selected for the synthesis. The synthesized compounds were subjected to TLC, melting point determination, FTIR, 1H NMR, 13C NMR and mass spectral analysis. The newly synthesized compounds were investigated for in vitro antitubercular eva

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Pais, João P., Olha Antoniuk, David Pires, et al. "Synthesis, Activity, Toxicity, and In Silico Studies of New Antimycobacterial N-Alkyl Nitrobenzamides." Pharmaceuticals 17, no. 5 (2024): 608. http://dx.doi.org/10.3390/ph17050608.

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Tuberculosis (TB) is a disease that plagues the frailest members of society. We have developed a family of N-alkyl nitrobenzamides that exhibit promising antitubercular activities and can be considered a structural simplification of known inhibitors of decaprenylphosphoryl-β-D-ribofuranose 2′-oxidase (DprE1), an essential Mycobacterium tuberculosis (Mtb) enzyme and an emergent antitubercular target. Hereby, we report the development of these compounds via a simple synthetic methodology as well as their stability, cytotoxicity, and antitubercular activity. Studying their in vitro activity revea

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Viswanathan, CL, and AV Shindikar. "Synthesis and in vitro antitubercular activity of 7-substituted fluoroquinolones." Indian Journal of Pharmaceutical Sciences 69, no. 2 (2007): 316. http://dx.doi.org/10.4103/0250-474x.33172.

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Puratchikody, Ayarivan, Ramalakshmi Natarajan, Mohanapriya Jayapal, and Mukesh Doble. "Synthesis, In Vitro Antitubercular Activity and 3D-QSAR of Novel Quinoxaline Derivatives." Chemical Biology & Drug Design 78, no. 6 (2011): 988–98. http://dx.doi.org/10.1111/j.1747-0285.2011.01246.x.

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Akalaeva, T. V., L. Yu Amel'kin, O. V. Baklanova, et al. "Antitubercular, antifungal, and antibacterial activity in vitro of 1-phenethylamino-1,2,3,4-tetrahydrocarbazoles." Pharmaceutical Chemistry Journal 24, no. 11 (1990): 826–29. http://dx.doi.org/10.1007/bf00768385.

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de Souza, Marcus V. N., Karla C. Pais, Carlos R. Kaiser, Mônica A. Peralta, Marcelle de L. Ferreira, and Maria C. S. Lourenço. "Synthesis and in vitro antitubercular activity of a series of quinoline derivatives." Bioorganic & Medicinal Chemistry 17, no. 4 (2009): 1474–80. http://dx.doi.org/10.1016/j.bmc.2009.01.013.

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Manvar, Atul T., Raghuvir R. S. Pissurlenkar, Vijay R. Virsodia, et al. "Synthesis, in vitro antitubercular activity and 3D-QSAR study of 1,4-dihydropyridines." Molecular Diversity 14, no. 2 (2009): 285–305. http://dx.doi.org/10.1007/s11030-009-9162-8.

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Banu, Saleha, Rajitha Bollu, Lingaiah Nagarapu, et al. "Design, Synthesis, and in vitro antitubercular activity of 1,2,3-triazolyl-dihydroquinoline derivatives." Chemical Biology & Drug Design 92, no. 1 (2018): 1315–23. http://dx.doi.org/10.1111/cbdd.13196.

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Tambe, Macchindra S., Sonali Gadhe, Amit Choudhari, Dhiman Sarkar, Jaiprakash N. Sangshetti, and Rajesh B. Patil. "Synthesis and Biological Evaluation of 3,4-Dihydro-2H-benzo[b][1,4]-oxazine-2-carboxylic Acid Derivatives as Antitubercular Agents." Asian Journal of Organic & Medicinal Chemistry 5, no. 2 (2020): 138–48. http://dx.doi.org/10.14233/ajomc.2020.ajomc-p261.

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A series of side chain modified structurally diverse 3,4-dihydro-2H-benzo[b][1,4]-oxazine-2-carboxylic acid derivatives were synthesized and characterized by IR, 1H NMR, 13C NMR and mass spectral study. All the newly synthesized compounds were examined for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Ra. The synthesized compounds exhibited minimum inhibitory concentration (IC50) ranging from 5.98 to >30 (μg/mL) against MtbH37Ra. Among the screened compounds, compounds 5a, 5c, 5d, 5f, 5g, 5h, 5I, 5j exhibited IC50 as 10.42, 11.81, 18.79, 5.98, 19.21, 24.81 and

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Watson, Daniel J., Lubbe Wiesner, Tlhalefo Matimela, Denzil Beukes, and Paul R. Meyers. "Tandem LC-MS Identification of Antitubercular Compounds in Zones of Growth Inhibition Produced by South African Filamentous Actinobacteria." Molecules 28, no. 11 (2023): 4276. http://dx.doi.org/10.3390/molecules28114276.

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Novel antitubercular compounds are urgently needed to combat drug-resistant Mycobacterium tuberculosis (Mtb). Filamentous actinobacteria have historically been an excellent source of antitubercular drugs. Despite this, drug discovery from these microorganisms has fallen out of favour due to the continual rediscovery of known compounds. To increase the chance of discovering novel antibiotics, biodiverse and rare strains should be prioritised. Subsequently, active samples need to be dereplicated as early as possible to focus efforts on truly novel compounds. In this study, 42 South African filam

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Patil, Akanksha V., Aishwarya R. Balap, Shailaja B. Jadhav, and Aarti V. Shingan. "Synthesis of Novel Mannich Bases of Indole and N-phenylaniline with its Molecular Docking, In silico Absorption, Distribution, Metabolism, and Excretion Profiling, In vitro Anti Tubercular Activity and Cytotoxicity Studies." Asian Journal of Pharmaceutical Research and Health Care 16, no. 4 (2024): 419–31. https://doi.org/10.4103/ajprhc.ajprhc_177_24.

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ABSTRACT Background: The bacillus Mycobacterium tuberculosis (MTB) is the major reason of the most infectious disease tuberculosis (TB). Regarding the past, it has ranked higher than human immunodeficiency virus/AIDS as the greatest source of death from a sole contagious disease for the past 5 years. The mannich reaction is a condensation of three molecules containing active hydrogen, an aldehyde, a primary or secondary amine, and one acidic hydrogen atom. Objective: This study illustrates the in silico physicochemical analysis, drug likeliness and toxicity prediction, synthesis, characterizat

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VAVAIYA, BHAVINKUMAR, SHIVANI PATEL, VRAJLAL PANSURIYA, VANITA MARVANIYA, and POPATBHAI PATEL. "In silico and In vitro Antitubercular Studies for Nitrogen Rich Hybrids of homopiperazine-pyrimidine-Pyrazole Adducts." Asian Journal of Chemistry 34, no. 3 (2022): 562–68. http://dx.doi.org/10.14233/ajchem.2022.23520.

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Novel homopiperazine-pyrimidine-pyrazole hybrids (3a-j) were synthesized using ethyl 2-cyanoacetate and 4,6-dichloropyrimidine as starting materials by a multi-step process to afford ethyl 5-amino-1-(6-chloropyrimidin-4-yl)-1H-pyrazole-4-carboxylate in good yields using polar protic media. The intermediate 1, in two steps, chloroamine condensation followed by acid amine coupling, furnished the title compounds ethyl 5-amino-1-(6-(4-substituted aryl-1,4-diazepan-1-yl)pyrimidin-4-yl)-1H-pyrazole-4-carboxylate (3a-j). The synthesized compounds were docked in the crystal structure of Mycobacterium

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Horita, Yasuhiro, Takemasa Takii, Tetsuya Yagi, et al. "Antitubercular Activity of Disulfiram, an Antialcoholism Drug, against Multidrug- and Extensively Drug-Resistant Mycobacterium tuberculosis Isolates." Antimicrobial Agents and Chemotherapy 56, no. 8 (2012): 4140–45. http://dx.doi.org/10.1128/aac.06445-11.

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ABSTRACTThe antimycobacterial activities of disulfiram (DSF) and diethyldithiocarbamate (DDC) against multidrug- and extensively drug-resistant tuberculosis (MDR/XDR-TB) clinical isolates were evaluatedin vitro. Both DSF and DDC exhibited potent antitubercular activities against 42 clinical isolates ofM. tuberculosis, including MDR/XDR-TB strains. Moreover, DSF showed remarkable bactericidal activityex vivoandin vivo. Therefore, DSF might be a drug repurposed for the treatment of MDR/XDR-TB.

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Xia, Yi, Yasheen Zhou, David S. Carter, et al. "Discovery of a cofactor-independent inhibitor ofMycobacterium tuberculosisInhA." Life Science Alliance 1, no. 3 (2018): e201800025. http://dx.doi.org/10.26508/lsa.201800025.

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New antitubercular agents are needed to combat the spread of multidrug- and extensively drug-resistant strains ofMycobacterium tuberculosis. The frontline antitubercular drug isoniazid (INH) targets the mycobacterial enoyl-ACP reductase, InhA. Resistance to INH is predominantly through mutations affecting the prodrug-activating enzyme KatG. Here, we report the identification of the diazaborines as a new class of direct InhA inhibitors. The lead compound, AN12855, exhibited in vitro bactericidal activity against replicating bacteria and was active against several drug-resistant clinical isolate

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Joshi, Shivam, and Neha Kawathekar. "Synthesis and Biological Evaluation of N-Benzylindolylchalcone Analogs as Antitubercular Agents." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 33, no. 03 (2023): 349. http://dx.doi.org/10.59467/ijhc.2023.33.349.

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A new series of N-benzylindolylchalcone analogs has been designed, synthesized, and screened for in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv. The synthesis of N-benzylatedindole-3-carbaldehyde derivatives, namely, -1-(2-methylbenzyl)-1H-indole-3-carbaldehyde (S2I1)1-(3-methylbenzyl)-1Hindole-3-carbaldehyde (S2I2), was achieved by N-benzylation of indole-3-carbaldehyde using a mixture of different bases in DMF. Subsequent condensation of these derivatives with various acetophenones led to the synthesis of the corresponding N-benzylindolylchalcone derivatives. Notab

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Jogul, Johnson, and Bharati Badami. "Sydnone derivatives as synthons for novel bismesoionic compounds. Synthesis of 3-(2-sulphido-1,3,4-thiadiazolium-4-carbonylphenyl) sydnones and 4-[4-(2-sulphido-1,3,4-thiadiazolium)benzoyl]- 1,3,4-thi." Journal of the Serbian Chemical Society 71, no. 8-9 (2006): 851–60. http://dx.doi.org/10.2298/jsc0609851j.

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Some hitherto unknown novel bismesoionic compounds, 3-[4/3 (5H/substituted- 2-sulphido-1,3,4-thiadiazolium-4 carbonyl)phenyl]sydnones 5a?d and 6a-d and 4-[4 (5H/substituted-2-sulphido-1,3,4-thiadiazolium)benzoyl] (5H/substituted-1,3,4-thiadiazolium- 2-thiolates 9a?d have been synthesized from 3-[(hydrazinocarbonyl)phenyl] sydnones 1 and 2. A few of these compounds exhibited in vitro antitubercular activity and also antimicrobial activity higher than the employed reference drugs.

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Mahnashi, Mater H., B. H. Prabhanjana, Sudarshan Seetammanavar, et al. "Synthesis and in silico studies of some new Schiff bases as antimicrobial and antitubercular agents." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 35, no. 01 (2025): 141. https://doi.org/10.59467/ijhc.2025.35.141.

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Ten pyridine carbohydrazide Schiff bases (3a-3e) and (5a-5e) were synthesized by refluxing pyridine carbohydrazides 1 and 4 with different ketones in the presence of ethanol and a few drops of glacial acetic acid. The synthesized compounds were biologically screened for antitubercular and antibacterial activity studies. The fit of these compounds within the active sites of the dihydrofolate reductase (DHFR) and enoyl ACP reductase was evaluated using molecular modeling techniques. The findings of the anticipated ADMET investigation showed that the compounds with the given names have drug-like

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