P.G. Department of Chemistry, New Arts, Science and Commerce College, University of Pune, Ahmednagar 414 003, India.
Bioorg Med Chem Lett. 2010 Sep 15;20(18):5572-6. doi: 10.1016/j.bmcl.2010.07.019. Epub 2010 Aug 17.
A series of fluorine containing 4-(substituted-2-hydroxybenzoyl) pyrazoles and pyrazolyl benzo[d]oxazoles were synthesized and evaluated for their antibacterial activity against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Bacillus subtilis and antifungal activity against Candida albicans. The antibacterial activities were expressed as the minimum inhibitory concentration (MIC50) in microg/ml. The compounds 1-(3,4-difluorophenyl)-4-(5-fluoro-2-hydroxybenzoyl)-1H-pyrazole (4b), oxime derivatives such as 1-(3,4-difluorophenyl)-1H-pyrazol-4-yl)(2-hydroxy-4-methylphenyl)methanone oxime (5b) and (5-chloro-2-hydroxyphenyl)(1-(3,4-difluorophenyl)-1H-pyrazol-4-yl)methanone oxime (5e) exhibited promising activities against tested bacterial strains. Except compound 1-(3,4-difluorophenyl)-4-(2-hydroxybenzoyl)-1H-pyrazole (4d), none of the other compounds showed promising antifungal activity.
一系列含氟的 4-(取代-2-羟基苯甲酰基)吡唑和吡唑并苯并[d]恶唑被合成，并评估了它们对金黄色葡萄球菌、大肠杆菌、铜绿假单胞菌和枯草芽孢杆菌的抗菌活性以及对白色念珠菌的抗真菌活性。抗菌活性用最小抑菌浓度（MIC50）表示，单位为微克/毫升。化合物 1-(3,4-二氟苯基）-4-(5-氟-2-羟基苯甲酰基）-1H-吡唑（4b）、肟衍生物如 1-(3,4-二氟苯基）-1H-吡唑-4-基）（2-羟基-4-甲基苯基）甲酮肟（5b）和（5-氯-2-羟基苯基）（1-(3,4-二氟苯基）-1H-吡唑-4-基）甲酮肟（5e）对测试的细菌菌株表现出有希望的活性。除了化合物 1-(3,4-二氟苯基）-4-(2-羟基苯甲酰基）-1H-吡唑（4d）外，其他化合物均没有表现出有希望的抗真菌活性。
