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Open AccessArticle

Anti-Tubercular Activity of Substituted 7-Methyl and 7-Formylindolizines and In Silico Study for Prospective Molecular Target Identification

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Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia
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Department of Biotechnology and Food Technology, Durban University of Technology, Durban 4001, South Africa
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Department of Microbiology, National Health Laboratory Services, KZN Academic Complex, Inkosi Albert Luthuli Central Hospital, Durban 4001, South Africa
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Department of Health Sciences, Faculty of Science, University of Mauritius, Réduit 80835 80832, Mauritius
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Department of Chemistry, Indian Institute of Science Education and Research Bhopal, Indore By-pass Road, Bhauri, Bhopal 462 066, Madhya Pradesh, India
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Department of Pharmacology, Faculty of Medicine, Minia University, El-Minia 61511, Egypt
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Department of Public Health Medicine, University of KwaZulu-Natal, Howard College Campus, Durban 4001, South Africa
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Institute for Stem Cell Biology and Regenerative Medicine, NCBS, TIFR, GKVK, Bellary Road, Bangalore 560 065, India
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Department of Pharmaceutical Sciences, College of Pharmacy, King Saud bin Abdulaziz University for Health Sciences, Riyadh 11481 11543, Saudi Arabia
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Authors to whom correspondence should be addressed.
Antibiotics 2019, 8(4), 247; https://doi.org/10.3390/antibiotics8040247
Received: 22 October 2019 / Revised: 27 November 2019 / Accepted: 29 November 2019 / Published: 3 December 2019
(This article belongs to the Section Novel Antimicrobial Agents)
Novel series of diversely substituted indolizines were designed, synthesized, and evaluated for their in vitro anti-mycobacterial activity against H37Rv and multi-drug-resistant (MDR) strains of Mycobacterium tuberculosis (MTB). Many compounds exhibited significant inhibitory activity against MTB H37Rv strains. Indolizines 2d, 2e, and 4 were also found to be active against MTB clinical isolates with multi-resistance to rifampicin and isoniazid. Indolizine 4 was identified as the most promising anti-mycobacterial agent, displaying minimum inhibitory concentration (MIC) values of 4 and 32 μg/mL against H37Rv and MDR strains, respectively. Furthermore, an in silico study was carried out for prospective molecular target identification and revealed favorable interactions with the target enzymes CYP 121, malate synthase, and DNA GyrB ATPase. None of the potent molecules presented toxicity against peripheral blood mononuclear (PBM) cell lines, demonstrating their potentiality to be used for drug-sensitive and drug-resistant tuberculosis therapy. View Full-Text
Keywords: indolizines; Mycobacterium tuberculosis; multi-drug resistance; molecular modeling; multi-component reaction; whole-cell anti-TB screening indolizines; Mycobacterium tuberculosis; multi-drug resistance; molecular modeling; multi-component reaction; whole-cell anti-TB screening
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MDPI and ACS Style

Venugopala, K.N.; Tratrat, C.; Pillay, M.; Mahomoodally, F.M.; Bhandary, S.; Chopra, D.; Morsy, M.A.; Haroun, M.; Aldhubiab, B.E.; Attimarad, M.; Nair, A.B.; Sreeharsha, N.; Venugopala, R.; Chandrashekharappa, S.; Alwassil, O.I.; Odhav, B. Anti-Tubercular Activity of Substituted 7-Methyl and 7-Formylindolizines and In Silico Study for Prospective Molecular Target Identification. Antibiotics 2019, 8, 247.

AMA Style

Venugopala KN, Tratrat C, Pillay M, Mahomoodally FM, Bhandary S, Chopra D, Morsy MA, Haroun M, Aldhubiab BE, Attimarad M, Nair AB, Sreeharsha N, Venugopala R, Chandrashekharappa S, Alwassil OI, Odhav B. Anti-Tubercular Activity of Substituted 7-Methyl and 7-Formylindolizines and In Silico Study for Prospective Molecular Target Identification. Antibiotics. 2019; 8(4):247.

Chicago/Turabian Style

Venugopala, Katharigatta N.; Tratrat, Christophe; Pillay, Melendhran; Mahomoodally, Fawzi M.; Bhandary, Subhrajyoti; Chopra, Deepak; Morsy, Mohamed A.; Haroun, Michelyne; Aldhubiab, Bandar E.; Attimarad, Mahesh; Nair, Anroop B.; Sreeharsha, Nagaraja; Venugopala, Rashmi; Chandrashekharappa, Sandeep; Alwassil, Osama I.; Odhav, Bharti. 2019. "Anti-Tubercular Activity of Substituted 7-Methyl and 7-Formylindolizines and In Silico Study for Prospective Molecular Target Identification" Antibiotics 8, no. 4: 247.

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