Development of 5-nitrothiazole derivatives: identification of leads against both replicative and latent Mycobacterium tuberculosis

Variam Ullas Jeankumar; Manoj Chandran; Ganesh Samala; Mallika Alvala; Pulla Venkat Koushik; Perumal Yogeeswari; Elena G Salina; Dharmarajan Sriram

doi:10.1016/j.bmcl.2012.10.060

Development of 5-nitrothiazole derivatives: identification of leads against both replicative and latent Mycobacterium tuberculosis

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7414-7. doi: 10.1016/j.bmcl.2012.10.060. Epub 2012 Oct 23.

Authors

Variam Ullas Jeankumar¹, Manoj Chandran, Ganesh Samala, Mallika Alvala, Pulla Venkat Koushik, Perumal Yogeeswari, Elena G Salina, Dharmarajan Sriram

Affiliation

¹ Antitubercular Drug Discovery Laboratory, Department of Pharmacy, Birla Institute of Technology& Science - Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, India.

PMID: 23137434
DOI: 10.1016/j.bmcl.2012.10.060

Abstract

Twenty eight 5-nitrothiazole derivatives were synthesized and evaluated for in vitro activities against Mycobacterium tuberculosis (MTB), cytotoxicity against HEK 293T. Among the compounds, 5-nitro-N-(5-nitrothiazol-2-yl)furan-2-carboxamide (20) was found to be the most active compound in vitro with MICs of 5.48 μM against log-phase culture of MTB and also non-toxic up to 100 μM.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anti-Bacterial Agents / chemical synthesis
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology*
Cell Proliferation / drug effects
Dose-Response Relationship, Drug
HEK293 Cells
Humans
Microbial Sensitivity Tests
Molecular Structure
Mycobacterium tuberculosis / drug effects*
Structure-Activity Relationship
Thiazoles / chemical synthesis
Thiazoles / chemistry
Thiazoles / pharmacology*

Substances

5-nitrothiazole
Anti-Bacterial Agents
Thiazoles