Development of 3-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel Mycobacterium tuberculosis pantothenate synthetase inhibitors
Development of 3-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel Mycobacterium tuberculosis pantothenate synthetase inhibitors
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DOI：
10.1016/j.ejmech.2013.08.036
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发表时间：
2013-11-01
影响因子：
6.7
通讯作者：
Sriram, Dharmarajan
中科院分区：
文献类型：
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作者：
Samala, Ganesh;Devi, Parthiban Brindha;Sriram, Dharmarajan
Forty 3-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives were synthesized from piperidin-4-one by five step synthesis and evaluated for Mycobacterium tuberculosis (MTB) pantothenate synthetase (PS) inhibition study, in vitro activities against MTB, cytotoxicity against RAW 264.7 cell line. Among the compounds, 1-benzoyl-N-(4-nitrophenyl)-3-phenyl-6,7-dihydro-1H-pyrazolo[4,3-c]pyridine-5(4H)-carboxamide (6ac) was found to be the most active compound with IC50 of 21.8 +/- 0.8 mu M against MTB PS, inhibited MTB with MIC of 26.7 mu M and it was non-cytotoxic at 50 RM. (C) 2013 Elsevier Masson SAS. All rights reserved.
