Antitubercular Drug Discovery Laboratory, Department of Pharmacy, Birla Institute of Technology and Science - Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, India.
Eur J Med Chem. 2013 Nov;69:356-64. doi: 10.1016/j.ejmech.2013.08.036. Epub 2013 Sep 12.
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 μM against MTB PS, inhibited MTB with MIC of 26.7 μM and it was non-cytotoxic at 50 μM.
合成了 43 个苯基-4,5,6,7-四氢-1H-吡唑并[4,3-c]吡啶衍生物，从哌啶-4-酮经过五步合成得到，并对分枝杆菌（MTB）泛酸合成酶（PS）抑制活性进行了评价，体外对 MTB 的活性和对 RAW 264.7 细胞系的细胞毒性。在这些化合物中，1-苯甲酰基-N-（4-硝基苯基）-3-苯基-6,7-二氢-1H-吡唑并[4,3-c]吡啶-5(4H)-甲酰胺（6ac）对 MTB PS 的抑制活性最强，IC₅₀为 21.8 ± 0.8 μM，对 MTB 的 MIC 为 26.7 μM，在 50 μM 时无细胞毒性。
