Seeking potent anti-tubercular agents: design and synthesis of substituted-N-(6-(4-(pyrazine-2-carbonyl)piperazine/homopiperazine-1-yl)pyridin-3-yl)benzamide derivatives as anti-tubercular agents

Author:

Srinivasarao Singireddi1234,Nandikolla Adinarayana1234,Suresh Amaroju1234,Calster Kevin Van56789,De Voogt Linda56789,Cappoen Davie56789,Ghosh Balaram10234,Aggarwal Himanshu1234,Murugesan Sankaranarayanan111024,Chandra Sekhar Kondapalli Venkata Gowri1234ORCID

Affiliation:

1. Department of Chemistry

2. Birla Institute of Technology and Science, Pilani

3. Hyderabad-500078

4. India

5. Department of Green Chemistry and Technology

6. Faculty of Bioscience Engineering

7. Ghent University

8. Ghent

9. Belgium

10. Department of Pharmacy

11. Medicinal Chemistry Research Laboratory

Abstract

We herein report 27 pyrazinamide analogues as anti-tubercular agents, of which six exhibited excellent activity with IC50 ≤ 2.18 μM and these were less toxic against HEK 293 cells.

Funder

Department of Biotechnology, Ministry of Science and Technology

Department of Science and Technology, Ministry of Science and Technology, India

Council of Scientific and Industrial Research, India

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemical Engineering,General Chemistry

Reference35 articles.

1. https://apps.who.int/iris/bitstream/handle/10665/311389/9789241550529-eng.pdf

2. https://www.atsjournals.org/doi/full/10.1164/rccm.167.4.603#readcube-epdf

3. Inhibition of M. tuberculosis in vitro in monocytes and in mice by aminomethylene pyrazinamide analogs

4. Synthesis and antimycobacterial evaluation of substituted pyrazinecarboxamides

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