Novel 1,3,4-oxadiazoles as antitubercular agents with limited activity against drug-resistant tuberculosis-Reference-Cited by-同舟云学术

Novel 1,3,4-oxadiazoles as antitubercular agents with limited activity against drug-resistant tuberculosis

Published:2019-03 Issue:6 Volume:11 Page:499-510
ISSN:1756-8919
Container-title:Future Medicinal Chemistry
language:en
Short-container-title:Future Medicinal Chemistry

Author:

Makane Vitthal B¹²,Krishna Vagolu Siva³,Krishna Eruva Vamshi²⁴,Shukla Manjulika⁵,Mahizhaveni Balakrishnan⁶,Misra Sunil²⁴,Chopra Sidharth⁵,Sriram Dharmarajan³,Azger Dusthackeer Vijayan N⁶,Rode Haridas B¹²

Affiliation:

1. Department of Organic Synthesis & Process Chemistry, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500 007, India

2. Academy of Scientific & Innovative Research, Ghaziabad, Uttar Pradesh 201002, India

3. Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Jawahar Nagar, Shameerpet Mandal, RR District, Hyderabad 500 078, India

4. Department of Biology, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India

5. Department of Microbiology, CSIR-Central Drug Research Institute, Lucknow 226021, Uttar Pradesh, India

6. Department of Bacteriology, National Institute for Research in Tuberculosis, Chennai, India

Abstract

Aim: In recent times, heterocyclic chemotypes are being explored for the development of new antimycobacterials that target the drug-resistant tuberculosis. Here, we are disclosing the 5-substitued 2-mercapto-1,3,4-oxadiazoles as potent antitubercular agents. Methodology: A small library of 2-mercapto-1,3,4-oxadiazoles was synthesized using various acids. The compounds were evaluated for antituberculosis activity against M. tuberculosis H37Rv. Results: Compound 8j was identified as antitubercular lead with MIC of 0.6 μg/ml against M. tuberculosis H37Rv. This compound was nontoxic to CHO-K1 cells and showed selectivity index of 39. Of note, 8j showed antitubercular activity against pre-extensively drug-resistant clinical isolate of Mycobacterium with MIC of 2 μg/ml. Conclusion: This study provides potent antitubercular agent which can be further optimized to discover novel antibiotics.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

Link

https://www.future-science.com/doi/pdf/10.4155/fmc-2018-0378

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