Discovery of Rimonabant and its potential analogues as anti-TB drug candidates
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 3.2...
Saved in:
Published in | Medicinal chemistry research Vol. 24; no. 7; pp. 2960 - 2971 |
---|---|
Main Authors | , , , , , , , |
Format | Journal Article |
Language | English |
Published |
New York
Springer US
01.07.2015
|
Subjects | |
Online Access | Get full text |
Cover
Loading…
Summary: | 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 µg/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.
Graphical Abstract |
---|---|
ISSN: | 1054-2523 1554-8120 |
DOI: | 10.1007/s00044-015-1346-4 |