<p>Design, synthesis and biological evaluation of indole and N-benzylated indole Mannich bases as potent antitubercular agents</p>
Online Publishing @ NISCAIR
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dc |
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Title Statement |
<p>Design, synthesis and biological evaluation of indole and N-benzylated indole Mannich bases as potent antitubercular agents</p> |
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Added Entry - Uncontrolled Name |
Kumar, M Murali Krishna; Pharmaceutical Chemistry Research Labs, AU College of Pharmaceutical Sciences, Andhra University, Visakahapatnam 530 003, India Namratha, J Risy ; Pharmaceutical Chemistry Research Labs, AU College of Pharmaceutical Sciences, Andhra University, Visakahapatnam 530 003, India Nagasree, K Purna ; Department of Pharmaceutical Chemistry, Vignan Institute of Pharmaceutical Technology, Duvvada, Visakahapatnam 530 003, India Sangeetha, G P V ; Pharmaceutical Chemistry Research Labs, AU College of Pharmaceutical Sciences, Andhra University, Visakahapatnam 530 003, India |
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Uncontrolled Index Term |
BM212 analogs, indole Mannich bases, pharmacophore, M. tuberculosis H37Rv, antitubercular |
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Summary, etc. |
<p style="text-align: justify;">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 <em>M. tuberculosis</em> <br /> H37Rv. We report here the synthesis, screening data and SAR studies of indole and substituted indole derivatives as antitubercular agents.</p> |
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Publication, Distribution, Etc. |
Indian Journal of Chemistry (IJC) 2022-02-21 00:00:00 |
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Electronic Location and Access |
application/pdf application/pdf http://op.niscair.res.in/index.php/IJC/article/view/60721 |
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Data Source Entry |
Indian Journal of Chemistry (IJC); ##issue.vol## 61, ##issue.no## 2 (2022): Indian Journal of Chemistry-(IJC) |
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Language Note |
en |
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