Development of 3-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel Mycobacterium tuberculosis pantothenate synthetase inhibitors

作者：Samala Ganesh; Devi Parthiban Brindha; Nallangi Radhika; Yogeeswari Perumal^*; Sriram Dharmarajan

来源：European Journal of Medicinal Chemistry, 2013, 69: 356-364.

DOI：10.1016/j.ejmech.2013.08.036

• Tuberculosis
• Pantothenate synthetase
• Cytotoxicity

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.

• 出版日期2013-11