Organic Chemistry Division, School of Advanced Sciences, VIT University, Vellore 632 014, India.
Eur J Med Chem. 2010 Mar;45(3):1173-80. doi: 10.1016/j.ejmech.2009.12.042. Epub 2009 Dec 28.
Novel 1,5-diaryl pyrazole derivatives viz. 5-(4-chlorophenyl)-1-(4-fluorophenyl)-1H-pyrazole-3-carboxamides (2a-e, 3, 3a-f), 2-(5-(4-chlorophenyl)-1-(4-fluorophenyl)-1H-pyrazole-3-yl)thiazoles (6a-c,7, 8, 9a-c, 10, 11) were synthesized by varying the active part (amide group) of pyrazole, characterized using IR, (1)H NMR, mass spectral data and screened for their antibacterial activity against Escherichia coli (ATTC-25922), Staphylococcus aureus (ATTC-25923), Pseudomonas aeruginosa (ATTC-27853), Klebsiella pneumonia. Similarly all these compounds were screened for their antifungal activity against Aspergillus flavus (NCIM No. 524), Aspergillus fumigates (NCIM No. 902), Penicillium marneffei and Trichophyton mentagrophytes. Interestingly all the synthesized compounds exhibited good antibacterial (except 2a-c, 8, 9a) and antifungal activity (except 2a-c, 6a, 8, 9a).
新型 1,5-二芳基吡唑衍生物，即 5-(4-氯苯基)-1-(4-氟苯基)-1H-吡唑-3-甲酰胺（2a-e、3、3a-f）、2-(5-(4-氯苯基)-1-(4-氟苯基)-1H-吡唑-3-基)噻唑（6a-c、7、8、9a-c、10、11），通过改变吡唑的活性部分（酰胺基）合成，用 IR、（1）H NMR、质谱数据进行了表征，并筛选了它们对大肠杆菌（ATTC-25922）、金黄色葡萄球菌（ATTC-25923）、铜绿假单胞菌（ATTC-27853）、肺炎克雷伯菌的抗菌活性。同样，所有这些化合物都被筛选出对黄曲霉（NCIM No. 524）、烟曲霉（NCIM No. 902）、马尔尼菲青霉和须癣毛癣菌的抗真菌活性。有趣的是，所有合成的化合物都表现出良好的抗菌（除了 2a-c、8、9a）和抗真菌活性（除了 2a-c、6a、8、9a）。
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