Joshi S D, Vagdevi H M, Vaidya V P, Gadaginamath G S
Department of Pharmaceutical Chemistry, S.E.T's College of Pharmacy, S.R. Nagar, Dharwad, Karnataka, India.
Eur J Med Chem. 2008 Sep;43(9):1989-96. doi: 10.1016/j.ejmech.2007.11.016. Epub 2007 Dec 5.
In the present study, a novel series of 4-pyrrol-1-yl benzoic acid hydrazide analogs, some derived 5-substituted-2-thiol-1,3,4-oxadiazoles, 5-substituted-4-amino-1,2,4-triazolin-3-thione and 2,5-dimethyl pyrroles have been synthesized in good yields and characterized by IR, NMR, mass spectral and elemental analyses. Compounds were evaluated for their preliminary in vitro antibacterial activity against some Gram-positive and Gram-negative bacteria and compounds were screened for antitubercular activity against Mycobacterium tuberculosis H37Rv strain by broth dilution assay method. Some compounds showed very good antibacterial and antitubercular activities.
在本研究中，已合成了一系列新型的4-吡咯-1-基苯甲酸酰肼类似物、一些衍生的5-取代-2-硫醇-1,3,4-恶二唑、5-取代-4-氨基-1,2,4-三唑啉-3-硫酮和2,5-二甲基吡咯，产率良好，并通过红外光谱、核磁共振、质谱和元素分析进行了表征。对化合物针对一些革兰氏阳性和革兰氏阴性细菌的初步体外抗菌活性进行了评估，并通过肉汤稀释法筛选了化合物针对结核分枝杆菌H37Rv菌株的抗结核活性。一些化合物表现出非常好的抗菌和抗结核活性。
