发现新型抗结核 1,5-二甲基-2-苯基-4-([5-(芳氨基)-1,3,4-恶二唑-2-基]甲氨基)-1,2-二氢-3H-吡唑-3-酮类似物。
Discovery of novel antitubercular 1,5-dimethyl-2-phenyl-4-([5-(arylamino)-1,3,4-oxadiazol-2-yl]methylamino)-1,2-dihydro-3H-pyrazol-3-one analogues.
机构信息
New Drug Discovery Research, Department of Pharmaceutical Chemistry, Alwar Pharmacy College, Alwar, Rajasthan 301 030, India; Department of Pharmaceutical Sciences, National Institute of Medical Sciences University, Jaipur, Rajasthan 303 121, India.
出版信息
Bioorg Med Chem Lett. 2012 Jan 15;22(2):969-72. doi: 10.1016/j.bmcl.2011.12.014. Epub 2011 Dec 8.
In search of potential therapeutics for tuberculosis, we describe herewith the synthesis, characterization and antimycobacterial activity of 1,5-dimethyl-2-phenyl-4-([5-(arylamino)-1,3,4-oxadiazol-2-yl]methylamino)-1,2-dihydro-3H-pyrazol-3-one analogues. Among the synthesized compounds, 4-[(5-[(4-fluorophenylamino]-1,3,4-oxadiazol-2-yl)methylamino]-1,2-dihydro-1,5-dimethyl-2-phenylpyrazol-3-one (4a) was found to be the most promising compound active against Mycobacterium tuberculosis H(37)Rv and isoniazid resistant M. tuberculosis with minimum inhibitory concentrations, 0.78 and 3.12μg/mL, respectively, free from any cytotoxicity (>62.5μg/mL).
在寻找结核病潜在治疗药物的过程中，我们在此描述了 1,5-二甲基-2-苯基-4-([5-(芳氨基)-1,3,4-恶二唑-2-基]甲氨基)-1,2-二氢-3H-吡唑-3-酮类似物的合成、表征和抗分枝杆菌活性。在所合成的化合物中，4-[(5-[(4-氟苯氨基]-1,3,4-恶二唑-2-基)甲氨基]-1,2-二氢-1,5-二甲基-2-苯基吡唑-3-酮（4a）对结核分枝杆菌 H(37)Rv 和异烟肼耐药结核分枝杆菌表现出最有希望的活性，其最低抑菌浓度分别为 0.78 和 3.12μg/mL，且无任何细胞毒性（>62.5μg/mL）。
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