Shaharyar Mohammad, Siddiqui Anees Ahamed, Ali Mohamed Ashraf, Sriram Dharmarajan, Yogeeswari Perumal
Faculty of Pharmacy, Jamia Hamdard University, Department of Pharmaceutical Chemistry, Hamdard Nagar, New Delhi-110062, India.
Bioorg Med Chem Lett. 2006 Aug 1;16(15):3947-9. doi: 10.1016/j.bmcl.2006.05.024. Epub 2006 May 24.
A series of N1-nicotinoyl-3- (4'-hydroxy-3'-methyl phenyl)-5-(substituted phenyl)-2-pyrazolines were synthesized by the reaction between isoniazid (INH) and chalcones and were tested for their antimycobacterial activity in vitro against Mycobacterium tuberculosis H37Rv (MTB) and INH-resistant M. tuberculosis (INHR-MTB) using the agar dilution method. Among the synthesized compounds, compound (i) N1-nicotinyl-3-(4'-hydroxy-3'-methyl phenyl)-5-(1''-chlorophenyl)-2-pyrazoline was found to be the most active agent against MTB and INHR-MTB, with minimum inhibitory concentration of 0.26 microm. When compared to INH-compound i was found to be 2.8- and 43.7-fold more active against MTB and INHR-MTB, respectively.
通过异烟肼（INH）与查耳酮之间的反应合成了一系列N1-烟酰基-3-（4'-羟基-3'-甲基苯基）-5-（取代苯基）-2-吡唑啉，并采用琼脂稀释法对其体外抗结核分枝杆菌H37Rv（MTB）和耐异烟肼结核分枝杆菌（INHR-MTB）的抗菌活性进行了测试。在合成的化合物中，化合物（i）N1-烟酰基-3-（4'-羟基-3'-甲基苯基）-5-（1''-氯苯基）-2-吡唑啉被发现是对MTB和INHR-MTB活性最强的药物，最低抑菌浓度为0.26微摩尔。与INH相比，化合物i对MTB和INHR-MTB的活性分别高2.8倍和43.7倍。
