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Journal articles on the topic 'Antitubercular'

Author: Grafiati

Published: 4 June 2021

Last updated: 1 February 2022

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1

Zitko, Jan, and Martin Doležal. "Old Drugs and New Targets as an Outlook for the Treatment of Tuberculosis." Current Medicinal Chemistry 25, no. 38 (January 7, 2019): 5142–67. http://dx.doi.org/10.2174/0929867324666170920154325.

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Background: Despite of the globally positive trends in the epidemiology of tuberculosis, the increasing rates of drug-resistant strains are urging to introduce new antituberculars into clinical practice. Development of a new chemical entity from hit to marketed drug is an extremely time and resources consuming process with uncertain outcome. Repurposing of clinically used drugs can be a cheaper alternative to develop new drugs effective in the treatment of tuberculosis. Objective: To extract the latest information on new mechanisms of action described or proposed for clinically used antitubercular drugs. To identify drugs from various pharmacodynamic groups as candidates for repurposing to become effective in combatting tuberculosis. Attention will be paid to elucidate the connection between repurposed drugs and new antituberculars in clinical practice or in clinical trials. Methods: Scientific databases were searched for the keywords. Results: We reviewed the latest aspects of usage and new mechanisms of action for both first-line and second-line antitubercular drugs in clinical practice. Further, we found that surprisingly large number of clinically used drugs from various pharmacodynamic groups have potential to be used in the treatment of tuberculosis, including antimicrobial drugs not typically used against tuberculosis, statins, CNS drugs (tricyclic phenothiazines, antidepressants, anticonvulsants), non-steroidal anti-inflammatory drugs, kinase inhibitors, and others (metformin, disulfiram, verapamil, lansoprazole). Repurposed drugs may become effective antituberculars, acting either by direct effects on mycobacteria or as adjunct, host-directed therapy. Conclusion: In this review, we showed that proper research of old drugs is a very efficient tool to develop new antituberculars.

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2

&NA;. "Antitubercular interactions reviewed." Reactions Weekly &NA;, no. 524 (October 1994): 2. http://dx.doi.org/10.2165/00128415-199405240-00001.

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3

&NA;. "Modern antitubercular therapy." Inpharma Weekly &NA;, no. 731 (April 1990): 2–3. http://dx.doi.org/10.2165/00128413-199007310-00004.

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4

HUSAIN, Asif, Aftab AHMAD, Anil BHANDARI, and Veerma RAM. "ANTITUBERCULAR ACTIVITY OF SOME NEWER 6-PYRIDAZINONE DERIVATIVES." SOUTHERN BRAZILIAN JOURNAL OF CHEMISTRY 19, no. 19 (December 20, 2011): 17–23. http://dx.doi.org/10.48141/sbjchem.v19.n19.2011.22_2011.pdf.

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Two series of 6-pyridazinone derivatives (17-30) were synthesized and evaluated for antitubercular activities against the Mycobacterium tuberculosis H37Rv strain. The results indicated that among the synthesized compounds, 5-( 4-hydroxy-3-methoxybenzyl}-3-phenyl-1,6-dihydro-6-pyridazinone (23) showed good antitubercular activity. Three more compounds, (18, 25 & 27) were significant in their antitubercular action. The present study reveals the antitubercular potential of 6-pyridazinones.

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5

Kar, Sidhartha S., and Cinu A. Thomas. "Strategically Placed Trifluoromethyl Substituent in the Realm of Antitubercular Drug Design." Current Drug Therapy 14, no. 2 (August 27, 2019): 114–23. http://dx.doi.org/10.2174/1574885513666180906101732.

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Background:Fluorinated substituents have played, and continue to play an important role in antitubercular drug design. Nonetheless, previous works have indicated that organofluorines like –F, CF3, -OCF3, and CHF2 etc have been used to modulate the pharmacodynamic and pharmacokinetic behaviour of antitubercular agents. Among the fluorinated groups, trifluoromethyl (-CF3) substituent is a very familiar pharmacophore used widely in antitubercular research.Objective:This review assesses the development of selected trifluoromethyl group bearing antitubercular agents that are either in treatment or considered to be potential. The prime objective of the present investigation was to provide initial evidences for the hypothesis that addition of trifluoromethyl group to antiTB agents could improve their potency. We also aimed to contribute to a better understanding of the role of trifluoromethyl group on drug-likeness antitubercular activity.Methods:In this review, we first brief out the possible effect of –CF3 substituent on pharmacodynamic and pharmacokinetic properties of drugs. Next, we turn to emphasize on the effect of trifluoromethyl substituent on different antitubercular scaffolds. Finally, we open the topic for the researchers to design potential antitubercular agents suitably substituted with fluorinated groups.Results:This review suggests that the replacement of –CF3 group in heterocyclic as well as phenyl ring led to the improvement in pharmacodynamic and pharmacokinetic properties of the compounds. Hence it's not surprising to see –CF3 group emerging as an alternative electron withdrawing group instead of halogens in many promising antitubercular agents.Conclusion:This unusual spectrum of advantage allied with its lipophilicity enhancing effect, made –CF3 group distinct from other substituents in modern antitubercular drug design. The present study provides conceptual advances to the understanding of the physicochemical properties of –CF3 group and its effect on antitubercular activity.

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6

K, Ishwar Bhat, and Abhishek Kumar. "PYRAZOLINES AS POTENT ANTITUBERCULAR AND CYTOTOXIC AGENTS." Asian Journal of Pharmaceutical and Clinical Research 10, no. 6 (June 1, 2017): 247. http://dx.doi.org/10.22159/ajpcr.2017.v10i6.17344.

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Objective: Pyrazolines are known to exhibit different biological and pharmacological properties such as anticancer, antibacterial, antifungal and antitubercular activities. Chalcones with an enone group between two aromatic rings exhibit remarkable pharmacological activities such as antiinflammatory, antibacterial, antitumor, antifungal, and antimalarial activity. A series of pyrazolines from chalcones have been synthesized and evaluated for antitubercular and cytotoxic activity studies.Methods: Chalcones [3-substituted phenyl-1-(p-tolyl)prop-2-en-1-one] were synthesized from various substituted aldehydes and 4-methyl acetophenone and cyclized into pyrazolines [5-substituted phenyl-3-(p-tolyl)-4,5-dihydro-1H-pyrazole] using hydrazine hydrate. Antitubercular and cytotoxic activity studies were carried out.Results: Antitubercular and cytotoxic activity studies of synthesized pyrazoline revealed that some compounds have showed promising activity.Conclusion: The observed results proved that pyrazolines are found to be interesting lead molecules for further synthesis as antitubercular and cytotoxic agents.

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7

Bakshi, S., M. Kaur, N. Saini, AA Mir, A. Duseja, SK Sinha, and S. Sharma. "Altered expressions of circulating microRNAs 122 and 192 during antitubercular drug induced liver injury indicating their role as potential biomarkers." Human & Experimental Toxicology 40, no. 9 (March 17, 2021): 1474–84. http://dx.doi.org/10.1177/0960327121997975.

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Drug induced liver toxicity is a serious health complication leading to high mortality rates and post marketing withdrawal of drugs. Although considered to be the gold standard biomarkers; aspartate aminotransferase, alanine aminotransferase, total bilirubin and alkaline phosphatase have been found to have specificities beyond liver, therefore more specific and predictive markers for the detection of antitubercular drug mediated liver damage are required. Unfortunately, the effectiveness of currently used first line antitubercular drugs namely isoniazid, rifampicin, pyrazinamide is often accompanied with liver injury, impeding the cure of patients. Keeping in view, the prognostic and diagnostic applications of microRNAs in various diseases, we tried to assess the importance of microRNAs 122 and 192 in antitubercular drug associated liver injuries. The study included subjects having tuberculosis of any type with antitubercular drug induced liver injury; naïve or newly diagnosed tuberculosis patients, tuberculosis patients on drugs not having toxicity and healthy controls. Observations from this study revealed that expression levels of miR-122 and miR-192 were significantly decreased in the serum of antitubercular drug induced liver injury patients only. Therefore, these microRNAs or the pathways associated with them can be used as a tool to predict or cure antitubercular drug associated liver injury in future.

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8

Durand, Francois, Gilles Jebrak, Dominique Pessayre, Michel Fournier, and Jacques Bernuau. "Hepatotoxicity of Antitubercular Treatments." Drug Safety 15, no. 6 (December 1996): 394–405. http://dx.doi.org/10.2165/00002018-199615060-00004.

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9

Wang, Lishu, Jungfeng Wang, Juan Liu, and Yonghong Liu. "Antitubercular Marine Natural Products." Current Medicinal Chemistry 25, no. 20 (June 14, 2018): 2304–28. http://dx.doi.org/10.2174/0929867324666170113120221.

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Due to the importance of nature as a source of new drug candidates, the purpose of this article is to emphasize the marine natural products, which exhibit antitubercular activity, published between January 2000 and May 2016, with 138 quotations to 250 compounds obtained from marine resources. These metabolites are organized by chemical constitution and named as simple alkyl lipids derivatives, aromatics derivatives, peptides, alkaloids, terpenoids, steroids, macrolides, and polycyclic polyketides.

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10

de Oliveira Viana, Jessika, Hamilton Mitsugu Ishiki, Marcus Tullius Scotti, and Luciana Scotti. "Multi-Target Antitubercular Drugs." Current Topics in Medicinal Chemistry 18, no. 9 (July 31, 2018): 750–58. http://dx.doi.org/10.2174/1568026618666180528124414.

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Tuberculosis is an infectious disease caused by Mycobacterium tuberculosis, which has high levels of mortality worldwide and has already gained resistance to first- and second-line drugs. The study by new chemical entities with promising activities becomes paramount to broaden the therapeutic strategies in the cure of the patients affected with this disease. In this context, in this review we report the discovery of 3 classes of compounds that can simultaneously interact with more than one target of Mycobacterium tuberculosis.

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11

Singanamala, Bhanudeep, Lokesh Saini, Priyanka Madaan, Paramjeet Singh, Pankaj C. Vaidya, and Jitendra Kumar Sahu. "Antitubercular therapy-induced psychosis." Neurology 93, no. 23 (December 2, 2019): 1012–13. http://dx.doi.org/10.1212/wnl.0000000000008578.

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12

Warman, A. J., T. S. Rito, N. E. Fisher, D. M. Moss, N. G. Berry, P. M. O'Neill, S. A. Ward, and G. A. Biagini. "Antitubercular pharmacodynamics of phenothiazines." Journal of Antimicrobial Chemotherapy 68, no. 4 (December 9, 2012): 869–80. http://dx.doi.org/10.1093/jac/dks483.

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13

Gu, Jian-Qiao, Yuehong Wang, Scott G. Franzblau, Gloria Montenegro, Danzhou Yang, and Barbara N. Timmermann. "Antitubercular Constituents ofValeriana laxiflora." Planta Medica 70, no. 6 (June 2004): 509–14. http://dx.doi.org/10.1055/s-2004-827149.

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14

Yadav, Smriti, Bharath Kumar Inturi, Shrinidhi B.R, Pooja H.J, Neenu Ganesh, and Gurubasavaraj V. Pujar. "Design, Synthesis and Antitubercular Evaluation of New Benzimidazole Scaffolds." Anti-Infective Agents 18, no. 4 (January 4, 2021): 375–83. http://dx.doi.org/10.2174/2211352518666200108091454.

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Background: To overcome one of the resistance mechanisms of Isoniazid (INH), there is a need for an antitubercular agent that can inhibit InhA enzyme by circumventing the formation of INH-NAD+ adduct. Objective: The objective of the study is the development of novel antitubercular agents that target Mycobacterium tuberculosis InhA (Enoyl Acyl Carrier Protein Reductase). Methods: A small-molecule chemical library was used for the identification of the novel InhA inhibitors using primary screening and molecular docking studies followed by the scaffold hopping approach. The designed molecules, 2-(2-(hydroxymethyl)-1H- benzo[d] imidazole-1-yl)- N- substituted acetamides were synthesized by reacting (1H- benzo[d]imidazole -2-yl)methanol with appropriate 2-chloro-N-substituted acetamides / dialkylamino carbonyl chlorides respectively in good yields (42-65%). The antitubercular activity of synthesized compounds was determined by Microplate Alamar Blue Assay (MABA) against Mycobacterium tuberculosis H37Rv strain. The selected compounds were screened for cytotoxicity on normal cell lines. Results: The antitubercular activity data revealed that the 4-chlorophenyl substituted derivative (3b) showed good MIC value at 6.25 μg/mL and, dimethylacetamide substituted derivative (3i) showed MIC at 25 μg/mL among the tested compounds. The substitution of dimethylacetamide (3i) group on the 1st position of benzimidazole has good antitubercular activity (25μg/mL) in comparison to the diethyl acetamide group (3j, 100μg/mL). Conclusion: The antitubercular activity data indicated that the tested compounds exhibited well to moderate inhibition of the H37Rv strains. The compounds (3b) with electronegative substitution on the phenyl moiety exhibited better antitubercular activity than that of the other substitutions. The active compounds have displayed a good safety profile on normal cell lines.

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15

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 have considerable binding score with enoyl ACP reductase enzyme of Mycobacterium tuberculosis. All the synthesized compounds were evaluated for antitubercular potential against Drug Resistant Mycobacterium tuberculosis H37Rv strain by Luciferase reporter assay method. Most of the synthesized compounds exhibited remarkable antitubercular potential against resistant strain.

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16

Sellamuthu, Satheeshkumar, Mohammad F. Bhat, Ashok Kumar, Gopal Nath, and Sushil K. Singh. "Design, Synthesis and Biological Evaluation of Carbazole Derivatives as Antitubercular and Antibacterial Agents." Current Bioactive Compounds 15, no. 1 (February 6, 2019): 83–97. http://dx.doi.org/10.2174/1573407214666180226125501.

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Background:The neuroleptic chlorpromazine has been reported for antitubercular activity but the associated antipsychotic activity restricted its clinical presentation.Objectives:Novel derivatives of carbazole having structural similarity with chlorpromazine were designed, in an attempt to reduce the associated side effects, while retaining the antitubercular activity.Materials and Methods:The designed molecules were synthesized and screened for antitubercular and antibacterial activities. The blood-brain barrier (BBB) permeability and mammalian cell (VERO) cytotoxicity (CC50) were examined to determine the safety of compounds.Results:Among the developed compounds, 14c, 15c, 16c and 17c were found to be promising against Mtb H37Rv at MIC of 1.56 &#181;g/ml. They were also effective against S. aureus and E. coli at MIC of 0.98 and 7.81 &#181;g/ml, respectively. The BBB permeability of the compounds was found to be less than chlorpromazine. Therefore, the developed compounds are expected to have diminished antipsychotic effect. The compounds were further marked safe against mammalian VERO cells at CC50 > 90 &#181;g/ml.Conclusion:The profound antitubercular activity with a concomitant reduction in BBB permeability of carbazole derivatives can pave new vista in the discovery of antitubercular drugs.

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17

Shaikh, Sameer I., Zahid Zaheer, Santosh N. Mokale, and Deepak K. Lokwani. "DEVELOPMENT OF NEW PYRAZOLE HYBRIDS AS ANTITUBERCULAR AGENTS: SYNTHESIS, BIOLOGICAL EVALUATION AND MOLECULAR DOCKING STUDY." International Journal of Pharmacy and Pharmaceutical Sciences 9, no. 10 (November 1, 2017): 50. http://dx.doi.org/10.22159/ijpps.2017v9i11.20469.

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Objective: synthesis of new 1, 3-diphenyl pyrazole derivatives 9(a-f) and 10(a-f) using molecular hybridization approach for antitubercular and cytotoxic studies.Methods: The structures of synthesized compounds were confirmed by 1H-NMR, 13C-NMR and mass spectra’s. The antitubercular activity of compounds and standard drugs were assessed against Mycobacterium tuberculosis using microplate Alamar Blue assay (MABA). The cytotoxic activities were performed by Sulforhodamine B (SRB) assay. The molecular docking and in silico ADME prediction were studied by using Schrodinger.Results: The results reveals that the compounds 9c, 9d, 10c and 10d exhibited substantial antitubercular potential with MIC < 20 μM. The cytotoxic studies revealed that the active compounds (9d, 10a, and 10d) are non-toxic to HeLa cancer cell lines with selectivity index >10. The molecular docking study was performed to study the binding orientation and affinity of synthesized compounds for InhA enzyme.Conclusion: The study explored that the 1, 3-diphenyl pyrazole hybrids coupled with well known antitubercular drugs could be a potential lead for antitubercular agents. In-silico molecular docking study helps to identify their corresponding intermolecular ligand-protein interactions with target enzyme. Also ADME prediction studies revealed that the compounds were in acceptable range to have pharmacokinetic parameters.

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18

Alghamdi, Saad, Shaheed Ur Rehman, Nashwa Talaat Shesha, Hani Faidah, Muhammad Khurram, and Sabi Ur Rehman. "Promising Lead Compounds in the Development of Potential Clinical Drug Candidate for Drug-Resistant Tuberculosis." Molecules 25, no. 23 (December 2, 2020): 5685. http://dx.doi.org/10.3390/molecules25235685.

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According to WHO report, globally about 10 million active tuberculosis cases, resulting in about 1.6 million deaths, further aggravated by drug-resistant tuberculosis and/or comorbidities with HIV and diabetes are present. Incomplete therapeutic regimen, meager dosing, and the capability of the latent and/or active state tubercular bacilli to abide and do survive against contemporary first-line and second line antitubercular drugs escalate the prevalence of drug-resistant tuberculosis. As a better understanding of tuberculosis, microanatomy has discovered an extended range of new promising antitubercular targets and diagnostic biomarkers. However, there are still no new approved antitubercular drugs of routine therapy for several decades, except for bedaquiline, delamanid, and pretomanid approved tentatively. Despite this, innovative methods are also urgently needed to find potential new antitubercular drug candidates, which potentially decimate both latent state and active state mycobacterium tuberculosis. To explore and identify the most potential antitubercular drug candidate among various reported compounds, we focused to highlight the promising lead derivatives of isoniazid, coumarin, griselimycin, and the antimicrobial peptides. The aim of the present review is to fascinate significant lead compounds in the development of potential clinical drug candidates that might be more precise and effective against drug-resistant tuberculosis, the world research looking for a long time.

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19

Narendhar, Bandi, Veerachamy Alagarsamy, and Chitra Krishnan. "Design and Synthesis of Novel 1-substituted-3-(3-(3-nitrophenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-yl amino) Isothioureas for their Anti-HIV, Antibacterial Activities, Graph Theoretical Analysis, Insilico Modeling, Prediction of Toxicity and Metabolic Studies." Drug Research 70, no. 08 (June 19, 2020): 348–55. http://dx.doi.org/10.1055/a-0991-7617.

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AbstractIn the present study, we have placed the substituted thiosemicarbazide moiety at the C-2 position and 3-nitrophenyl group at N-3 position of benzopyrimidines and studied their antitubercular, anti-HIV and antibacterial activities against selected gram positive and negative bacteria. The target compounds 1-substituted-3-(3-(3-nitrophenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-ylamino) isothioureas (PTS1 – PTS15 ) were obtained by the reaction of 2-hydrazino-3-(3-nitrophenyl) benzopyrimidin-4(3 H)-one (5) with different alkyl/aryl isothiocyanates followed by methylation with dimethyl sulphate. All synthesized compounds were screened for their antitubercular, anti-HIV and antibacterial activity against selective gram positive and gram negative bacteria by agar dilution method. Among the series, compound 2-methyl-3-(3-(3-nitrophenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-ylamino)-1-(3-chlorophenyl)isothiourea (PTS14) shown most potent activity against Klebsiella pneumoniae, Proteus vulgaris and Staphylococcus aureus; PTS14 exhibited the antitubercular activity at the minimum microgram of 1.56 µg/mL and anti-HIV activity at 0.96 µg/mL against HIV1 and HIV2 and offers potential for further optimization and development to new antitubercular and anti-HIV agents. The results obtained from this study confirm that the synthesized and biologically evaluated benzopyrimidines showed promising antimicrobial, antitubercular and anti-HIV activities and are new scaffolds for antimicrobial activity.

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20

Pathak, U. N., B. O. Shrestha, and R. R. Shrestha. "PYRAZINAMIDE INDUCED ACUTE GOUTY ARTHRITIS." Journal of Nepal Medical Association 41, no. 143 (January 1, 2003): 408–10. http://dx.doi.org/10.31729/jnma.788.

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A typical case of pyrazinamide induced acute gouty arthritis in a tuberculous patientwith antitubercular therapy including pyrazinamide was reported. It highlights theneed of awareness among physicians about the potentially morbid complications ofpyrazinamide. The other antitubercular drug like ethambutol may also cause increasein serum uric acid.Key Words: Gout, Pyrazinamide.

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21

&NA;. "Antitubercular ADR rate 'acceptably low'." Reactions Weekly &NA;, no. 592 (March 1996): 4. http://dx.doi.org/10.2165/00128415-199605920-00007.

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22

Ahirrao, Pallavi. "Recent Developments in Antitubercular Drugs." Mini-Reviews in Medicinal Chemistry 8, no. 14 (December 1, 2008): 1441–51. http://dx.doi.org/10.2174/138955708786786516.

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23

&NA;. "Antitubercular ADRs in pulmonary tuberculosis." Reactions Weekly &NA;, no. 631 (December 1996): 5. http://dx.doi.org/10.2165/00128415-199606310-00008.

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24

Matzke, Gary R., Michael H. Schwenk, and William F. Keane. "Antifungal, Antitubercular, and Antiviral Agents." Seminars in Dialysis 1, no. 3 (October 1, 2007): 170–73. http://dx.doi.org/10.1111/j.1525-139x.1988.tb00752.x.

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&NA;. "Short-course antitubercular therapy effective." Inpharma Weekly &NA;, no. 1065 (November 1996): 12. http://dx.doi.org/10.2165/00128413-199610650-00023.

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26

Tiwari, Neerja, Jayprakash Thakur, Dharmendra Saikia, and Madan M. Gupta. "Antitubercular diterpenoids from Vitex trifolia." Phytomedicine 20, no. 7 (May 2013): 605–10. http://dx.doi.org/10.1016/j.phymed.2013.01.003.

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27

Zhang, Shengping, Iman Kavianinia, and Margaret A. Brimble. "Naturally occurring antitubercular cyclic peptides." Tetrahedron Letters 60, no. 50 (December 2019): 151339. http://dx.doi.org/10.1016/j.tetlet.2019.151339.

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Duncan, Ken, and Clifton E. Barry III. "Prospects for new antitubercular drugs." Current Opinion in Microbiology 7, no. 5 (October 2004): 460–65. http://dx.doi.org/10.1016/j.mib.2004.08.011.

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Kuneš, Jiřı́, Jaroslav Bažant, Milan Pour, Karel Waisser, Milan Šlosárek, and Jiřı́ Janota. "Quinazoline derivatives with antitubercular activity." Il Farmaco 55, no. 11-12 (December 2000): 725–29. http://dx.doi.org/10.1016/s0014-827x(00)00100-2.

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Li, Jinjing, Susan A. Bourne, Melgardt M. de Villiers, A. Michael Crider, and Mino R. Caira. "Polymorphism of the Antitubercular Isoxyl." Crystal Growth & Design 11, no. 11 (November 2, 2011): 4950–57. http://dx.doi.org/10.1021/cg200860p.

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31

Cardoso, Silvia H., Milena B. Barreto, Maria C. S. Lourenço, Maria das Graças M. de O. Henriques, André L. P. Candéa, Carlos R. Kaiser, and Marcus V. N. de Souza. "Antitubercular Activity of New Coumarins." Chemical Biology & Drug Design 77, no. 6 (April 19, 2011): 489–93. http://dx.doi.org/10.1111/j.1747-0285.2011.01120.x.

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32

Lee, Ae-Ra, Soo Jung Kim, Junghyun Kim, Ju-Hee Park, Jung-Kyu Lee, Ju-Young Kim, Suh-Young Lee, and Hye-Ryun Kang. "Successful desensitization for antitubercular drugs." Allergy, Asthma & Respiratory Disease 1, no. 4 (2013): 395. http://dx.doi.org/10.4168/aard.2013.1.4.395.

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Shah, Manish, Geoffrey Wells, Tracey Bradshaw, Charles Laughton, Malcolm Stevens, and Andrew Westwell. "Antitubercular Properties of Substituted Hydroxycyclohexadienones." Letters in Drug Design & Discovery 3, no. 6 (August 1, 2006): 419–23. http://dx.doi.org/10.2174/157018006777805486.

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Keri, Rangappa S., Siddappa A. Patil, Srinivasa Budagumpi, and Bhari Mallanna Nagaraja. "Triazole: A Promising Antitubercular Agent." Chemical Biology & Drug Design 86, no. 4 (February 19, 2015): 410–23. http://dx.doi.org/10.1111/cbdd.12527.

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Kumar, B., and K. Sandhu. "Erythema nodosum and antitubercular therapy." Journal of Dermatological Treatment 15, no. 4 (July 2004): 218–21. http://dx.doi.org/10.1080/09546630410033754.

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Gu, Jian-Qiao, Yuehong Wang, Scott G. Franzblau, Gloria Montenegro, and Barbara N. Timmermann. "Constituents ofSeneciochionophiluswith Potential Antitubercular Activity." Journal of Natural Products 67, no. 9 (September 2004): 1483–87. http://dx.doi.org/10.1021/np049831z.

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Lei, Benfang, Chih-Jen Wei, and Shiao-Chun Tu. "Action Mechanism of Antitubercular Isoniazid." Journal of Biological Chemistry 275, no. 4 (January 28, 2000): 2520–26. http://dx.doi.org/10.1074/jbc.275.4.2520.

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Wächter, Gerald A., Susanne Valcic, Scott G. Franzblau, Enrique Suarez, and Barbara N. Timmermann. "Antitubercular Activity of Triterpenoids fromLippiaturbinata." Journal of Natural Products 64, no. 1 (January 2001): 37–41. http://dx.doi.org/10.1021/np000267b.

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Asif, Mohammad, Anees A. Siddiqui, and Asif Husain. "Quinolone derivatives as antitubercular drugs." Medicinal Chemistry Research 22, no. 3 (June 12, 2012): 1029–42. http://dx.doi.org/10.1007/s00044-012-0101-3.

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40

Nilewar, S. S., and M. K. Kathiravan. "Mycothiol: A promising antitubercular target." Bioorganic Chemistry 52 (February 2014): 62–68. http://dx.doi.org/10.1016/j.bioorg.2013.11.004.

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41

Kumar, Atul, and Alka Kumar. "Relook hysteroscopy after antitubercular therapy." Fertility and Sterility 89, no. 3 (March 2008): 701–2. http://dx.doi.org/10.1016/j.fertnstert.2007.07.1346.

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Tonelli, Michele, Federica Novelli, Bruno Tasso, Anna Sparatore, Vito Boido, Fabio Sparatore, Sara Cannas, et al. "Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines." Bioorganic & Medicinal Chemistry 22, no. 24 (December 2014): 6837–45. http://dx.doi.org/10.1016/j.bmc.2014.10.035.

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Kumar, Sushil, Vinod Puri, M. M. Mehndiratta, Suvira Gupta, Ajay Bhutani, and Chaitanya Sharma. "Paradoxical response to antitubercular drugs." Indian Journal of Pediatrics 62, no. 6 (November 1995): 695–701. http://dx.doi.org/10.1007/bf02825120.

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Keri, Rangappa S., and Siddappa A. Patil. "Quinoline: A promising antitubercular target." Biomedicine & Pharmacotherapy 68, no. 8 (October 2014): 1161–75. http://dx.doi.org/10.1016/j.biopha.2014.10.007.

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Teixeira, Cátia, Cristina Ventura, José R. B. Gomes, Paula Gomes, and Filomena Martins. "Cinnamic Derivatives as Antitubercular Agents: Characterization by Quantitative Structure–Activity Relationship Studies." Molecules 25, no. 3 (January 21, 2020): 456. http://dx.doi.org/10.3390/molecules25030456.

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Tuberculosis, caused by Mycobacterium tuberculosis (Mtb), remains one of the top ten causes of death worldwide and the main cause of mortality from a single infectious agent. The upsurge of multi- and extensively-drug resistant tuberculosis cases calls for an urgent need to develop new and more effective antitubercular drugs. As the cinnamoyl scaffold is a privileged and important pharmacophore in medicinal chemistry, some studies were conducted to find novel cinnamic acid derivatives (CAD) potentially active against tuberculosis. In this context, we have engaged in the setting up of a quantitative structure–activity relationships (QSAR) strategy to: (i) derive through multiple linear regression analysis a statistically significant model to describe the antitubercular activity of CAD towards wild-type Mtb; and (ii) identify the most relevant properties with an impact on the antitubercular behavior of those derivatives. The best-found model involved only geometrical and electronic CAD related properties and was successfully challenged through strict internal and external validation procedures. The physicochemical information encoded by the identified descriptors can be used to propose specific structural modifications to design better CAD antitubercular compounds.

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Boukthir, Mouna, Zribi Fethi, Iman Halloum, Laurent Kremer, and Fakher Chabchoub. "Synthesis and Antitubercular Evaluation of Some Novel 1,2,3,6-tetrahydropyrimidine-5-carbonitrile." JOURNAL OF ADVANCES IN CHEMISTRY 9, no. 3 (December 1, 2013): 2072–77. http://dx.doi.org/10.24297/jac.v9i3.1014.

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In an attempt to find a new class of antitubercular agents, a series of 1,2,3,6-tetrahydropyrimidine-5-carbonitrile were prepared via the reaction of ethyl N-ethoxycarbonylbenzimidate 2a-b with cyanoacetanilide derivatives 1a-c. These compounds were screened for their antitubercular activity against M. tuberculosis. Several analogues, such as 2,6-dioxo-1-phenyl-4-p-tolyl-1,2,3,6-tetrahydropyrimidine-5-carbonitrile 3a, 1-benzyl-2, 6-dioxo-4-p-tolyl-1,2,3,6-tetrahydropyrimidine-5-carbonitrile 3c and 1-benzyl-2, 6-dioxo-4-phenyl-1,2,3,6-tetrahydropyrimidine-5-carbonitrile 3d exhibited a potent antitubercular activity with an MIC values ranging from 10-35 µg/ml. Structures of the newly synthesized compounds were established by spectral data and HRMS.

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Olga Mykolaivna Shvets, Olga Stanislavna Shevchenko, and Hanna Leonidivna Stepanenko. "INSULIN RESISTANCE IN DRUG-SUSCEPTIBLE PULMONARY TUBERCULOSIS PATIENTS DURING THE FIRST MONTH OF ANTITUBERCULAR TREATMENT." International Academy Journal Web of Scholar 1, no. 8(38) (August 31, 2019): 13–17. http://dx.doi.org/10.31435/rsglobal_wos/31082019/6650.

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The study was aimed to investigate insulin resistance development in drug-susceptible newly diagnosed pulmonary tuberculosis patients. Those patients who developed insulin resistance during the 30 days of antitubercular therapy have expressed metabolic changes, that may be associated with impaired liver function due to the toxic effects of antitubercular drugs.

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Shaik, Afzal B., Richie R. Bhandare, Srinath Nissankararao, Zehra Edis, N. Ravikiran Tangirala, Shaik Shahanaaz, and M. Mukhlesur Rahman. "Design, Facile Synthesis and Characterization of Dichloro Substituted Chalcones and Dihydropyrazole Derivatives for Their Antifungal, Antitubercular and Antiproliferative Activities." Molecules 25, no. 14 (July 13, 2020): 3188. http://dx.doi.org/10.3390/molecules25143188.

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Infectious diseases caused by fungi and mycobacteria pose an important problem for humankind. Similarly, cancer is one of the leading causes of death globally. Therefore, there is an urgent need for the development of novel agents to combat the deadly problems of cancer, tuberculosis, and also fungal infections. Hence, in the present study, we designed, synthesized, and characterized 30 compounds including 15 chalcones (2–16) and 15 dihydropyrazoles (17–31) containing dichlorophenyl moiety and also screened these compounds for their antifungal, antitubercular, and antiproliferative activities. Among these compounds, the dihydropyrazoles showed excellent antifungal and antitubercular activities whereas the chalcones exhibited promising antiproliferative activity. Among the dihydropyrazoles, compound 31 containing 2-thienyl moiety showed promising antifungal activity (MIC 5.35 µM), whereas compounds 22 and 24 containing 2,4-difluorophenyl and 4-trifluoromethyl scaffolds revealed significant antitubercular activity with the MICs of 3.96 and 3.67 µM, respectively. Compound 16 containing 2-thienyl moiety in the chalcone series showed the highest anti-proliferative activity with an IC50 value of 17 ± 1 µM. The most active compounds identified through this study could be considered as starting points in the development of drugs with potential antifungal, antitubercular, and antiproliferative activities.

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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 vivo activity of Mycobacterium tuberculosis shikimate kinase ( MtSK) inhibitors available in the literature. In this review, we present a summary of the progress of SK inhibitor discovery and evaluation with particular attention toward development of new antitubercular agents.

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Saxena, Anil K., and Muneer Alam. "ATP Synthase Inhibitors as Anti-tubercular Agents: QSAR Studies in Novel Substituted Quinolines." Current Topics in Medicinal Chemistry 20, no. 29 (November 20, 2020): 2723–34. http://dx.doi.org/10.2174/1568026620666200903163515.

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Background: Tuberculosis (TB) is a major infectious disease caused by Mycobacterium Tuberculosis. As per the World Health Organization (WHO) report of 2019, there were 1.5 million deaths in the year 2018, mainly because of multi- and extensively drug-resistant tuberculosis (MDR & XDR-TB). Among several antitubercular drugs in clinical trials, bedaquiline (TMC207) is a highly promising drug that was approved by the FDA in 2012 and marketed in 2016 for the treatment of multidrug resistant TB in combination with other drugs. Bedaquiline acts on mycobacterial ATP synthase and is highly effective in replicating as well as on dormant mycobacteria. Several series of substituted quinolines have been reported with their antitubercular and ATP synthase inhibitory activity. Methods: To understand the role of physicochemical parameters like hydrophobicity, electronic and steric factors in eliciting the biological response, the Quantitative structure-activity relationship (QSAR) studies have been carried out using the computed parameters as independent variable and activity (-log IC50/MIC) as the dependent variable. Results: The developed QSAR models in terms of positively contributing Molar Refractivity (MR) and negatively contributing Partition Coefficient (PC) and Connolly Molecular Area (CMA) parameters have high predictivity as also shown on external data set and the mean value of the computed 3D parameters of enantiomers may be used in QSAR analysis for racemic compounds. Conclusion: These results are also substantiated by pharmacophore modeling. The similar dependence of antitubercular activity against whole-cell M.Tb.H37Rv on MR and CMA suggests ATP synthase as the main target for antitubercular activity and the QSAR models may be useful in the identification of novel antitubercular agents.

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