Record Details

Design, synthesis and biological evaluation of indole and N-benzylated indole Mannich bases as potent antitubercular agents

NOPR - NISCAIR Online Periodicals Repository

View Archive Info
 
 
Field Value
 
Title Design, synthesis and biological evaluation of indole and N-benzylated indole Mannich bases as potent antitubercular agents
 
Creator Kumar, M Murali Krishna
Namratha, J Risy
Nagasree, K Purna
Sangeetha, G P V
 
Subject BM212 analogs
indole Mannich bases
pharmacophore
M. tuberculosis H37Rv
antitubercular
 
Description 210-224
Though effective medicines have been available for treating drug-susceptible tuberculosis infections, the chances go from bleak to null as we move from multidrug resistant (MDR) to extremely drug resistant (XDR) or totally drug resistant (TDR) disease. Coordinated efforts made by international community have resulted in the identification of a few important anti TB agents like BM212, SQ109, AZD5847 and Sutezolid which are in the late phases of clinical trials. After Rifampicin, only two drugs Bedaquiline (2013) and Delaminid (2014) have been approved for the treatment of tuberculosis. This clearly shows the need for new leads towards fighting tuberculosis. In our present work, we have synthesized a series of indole and substituted indole Mannich bases designed by using structural features of BM212. Further, these synthesized derivatives have been analyzed by IR, NMR and mass spectral studies and are screened for anti-tubercular and antimicrobial activity. Among these, 23 compounds have shown potent anti TB activity with a MIC ≤3.12 μg/mL against M. tuberculosis H37Rv. We report here the synthesis, screening data and SAR studies of indole and substituted indole derivatives as antitubercular agents.
 
Date 2022-02-15T11:39:57Z
2022-02-15T11:39:57Z
2022-02
 
Type Article
 
Identifier 2583-1321 (Online); 0019-5103 (Print)
http://nopr.niscair.res.in/handle/123456789/59187
 
Language en
 
Publisher NIScPR-CSIR, India
 
Source IJC Vol.61(02) [February 2022]