Gupta Preeti, Hameed Shahul, Jain Rahul
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar, Punjab 160 062, India.
Eur J Med Chem. 2004 Sep;39(9):805-14. doi: 10.1016/j.ejmech.2004.05.005.
We describe in vitro anti-Mycobacterium tuberculosis activities of ring-substituted-1H-imidazole-4-carboxylic acid derivatives (1-6), and 3-(2-alkyl-1H-imidazol-4-yl)-propionic acid derivatives (7-13) against drug-sensitive and drug-resistant M. tuberculosis H37Rv strains. The most effective analogues, 2f (R=R(1)=c-C(5)H(9)), and 2h (R=R(1)=c-C(6)H(11)) have produced >90% inhibition at a concentration of <6.25 microg/ml in the drug-sensitive screen. Upon further evaluation against drug-resistant strains, both analogues 2f and 2h produced an MIC value of 25.0 microg/ml. The observation of significant anti-tuberculosis activity in some of these analogues describes the discovery of novel ring-substituted-1H-imidazole-4-carboxylic acid ethyl esters as a new class of anti-tuberculosis agents.
我们描述了环取代-1H-咪唑-4-羧酸衍生物（1-6）和3-（2-烷基-1H-咪唑-4-基）-丙酸衍生物（7-13）对药物敏感和耐药结核分枝杆菌H37Rv菌株的体外抗结核活性。最有效的类似物2f（R = R(1)=环戊基）和2h（R = R(1)=环己基）在药物敏感筛选中，浓度<6.25微克/毫升时产生了>90%的抑制率。在对耐药菌株的进一步评估中，类似物2f和2h的最低抑菌浓度（MIC）值均为25.0微克/毫升。在其中一些类似物中观察到显著的抗结核活性，这表明发现了一类新型的环取代-1H-咪唑-4-羧酸乙酯作为新型抗结核药物。
