Benzo[d]thiazol-2-yl(piperazin-1-yl)methanones as new anti-mycobacterial chemotypes: Design, synthesis, biological evaluation and 3D-QSAR studies
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- 作者：Sahaj Pancholiaa ; Tejas M. Dhameliyaa ; Parth Shaha ; Pradeep S. Jadhavara ; Jonnalagadda Padma Sridevib ; Perumal Yogeshwarib ; Dharmarajan Sriramb ; Asit K. Chakrabortia ; akchakraborti@niper.ac.in" class="auth_mail" title="E-mail the corresponding author ; akchakraborti@rediffmail.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：Tuberculosis ; Benzo[d]thiazole-2-carboxamides ; New antibacterial chemotypes ; Anti-mycobacterial activity ; COMFA ; and 3D-QSAR
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：30 June 2016
- 年：2016
- 卷：116
- 期：Complete
- 页码：187-199
- 全文大小：1254 K
文摘
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36 compounds were synthesized using green synthetic protocol.
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Twenty-one compounds displayed good in vitro anti-mycobacterial activity.
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The most potent 3 compounds exhibited MIC of 0.78 μg/mL with therapeutic index >60.
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The 3D-QSAR for anti-TB compounds has been established with significant CoMFA model.