Yar Mohammad Shahar, Ali Mohamed Ashraf, Sriram Dharmarajan, Yogeeswari Perumal
Faculty of Pharmacy, Jamia Hamdard University, Department of Pharmaceutical Chemistry, Hamdard Nagar, New Delhi-110062, India.
Acta Pol Pharm. 2006 Nov-Dec;63(6):491-6.
A series of 3-(4'-hydroxy-3'-methylphenyl)-5-[(substituted) phenyl]-4,5-dihydro-1H-1-pyrazolyl-4-pyridylmethanone derivatives were synthesized by the reaction between isoniazid (INH) and various chalcones and were tested for their antimicrobial activity in vitro against Staphylococcus aureus 209p, Escherichia coli ESS 2231, Aspergillus fumigatus, Candida albicans, Candida albicans ATCC 10231, Candida krusei GO3 and Candida glabrata HO5. Among the synthesized compounds, all the compounds possess the significant antibacterial activity. Compounds I(III) and I(x), i.e. 3-(4'-hydroxy-3'-methylphenyl)-5-(4"-dimethylaminophenyl)-4,5-dihydro-1H-1-pyrazolyl-4-pyridyl methanone and 3-(4'-hydroxy-3'-methylphenyl)-5-(2",6"-dichlorophenyl)-4,5-dihydro-1H-1-pyrazolyl-4-pyridylmethanone were found to be the most active agents against used bacterial and fungal strains with minimum inhibitory concentration of less than 0.5 microg/mL and were equally active as standard drugs Ofloxacin and Fluconazole.
通过异烟肼（INH）与各种查尔酮之间的反应合成了一系列3-（4'-羟基-3'-甲基苯基）-5- [（取代）苯基] -4,5-二氢-1H-1-吡唑基-4-吡啶基甲酮衍生物，并对其体外抗金黄色葡萄球菌209p、大肠杆菌ESS 2231、烟曲霉、白色念珠菌、白色念珠菌ATCC 10231、克鲁斯念珠菌GO3和光滑念珠菌HO5的抗菌活性进行了测试。在合成的化合物中，所有化合物都具有显著的抗菌活性。化合物I（III）和I（x），即3-（4'-羟基-3'-甲基苯基）-5-（4''-二甲基氨基苯基）-4,5-二氢-1H-1-吡唑基-4-吡啶基甲酮和3-（4'-羟基-3'-甲基苯基）-5-（2''，6''-二氯苯基）-4,5-二氢-1H-1-吡唑基-4-吡啶基甲酮被发现是对所用细菌和真菌菌株最具活性的药剂，其最低抑菌浓度小于0.5微克/毫升，并且与标准药物氧氟沙星和氟康唑具有同等活性。
