Discovery of rimonabant and its potential analogues as anti-TB drug candidates

TitleDiscovery of rimonabant and its potential analogues as anti-TB drug candidates
Publication TypeJournal Article
Year of Publication2015
AuthorsGajbhiye, JM, More, NA, Patil, MD, Ummanni, R, Kotapalli, SS, Yogeeswari, P, Sriram, D, Masand, VH
JournalMedicinal Chemistry Research
Volume24
Issue7
Pagination2960-2971
Date PublishedJUL
ISSN1054-2523
KeywordsDiaryl pyrazoles, H37Rv, MTCYP-121, Mycobacterium tuberculosis, Rimonabant, tuberculosis
Abstract

Rimonabant and its analogues have been synthesized in moderate to good yields using a simple synthetic route. All the newly synthesized compounds were subjected to in vitro screening against M. tuberculosis and M. smegmatis. The most potent analogue JMG-14 exhibits MIC value of 3.13 compared to 3.25 and 50 A mu g/ml for ethambutol and pyrazinamide, respectively. The molecular docking reveals that pyrazole ring, number and position of halogen atoms play a crucial role in deciding interactions with MTCYP-121. These findings open up a new avenue in the search of potent anti-TB drugs with rimonabant and its novel analogue JMG-14 as lead molecules.

DOI10.1007/s00044-015-1346-4
Type of Journal (Indian or Foreign)

Foreign

Impact Factor (IF)

1.436

Divison category: 
Organic Chemistry