Prakash O, Hussain K, Aneja K R, Sharma C
Department of Chemistry, Kurukshetra University, Kurukshetra-136 119, India.
Indian J Pharm Sci. 2011 Sep;73(5):586-90. doi: 10.4103/0250-474X.99023.
Seven new 2-(3-(4-aryl)-1-phenyl-1H-pyrazol-4-yl) chroman-4-ones (4a-4g) have been synthesized by cyclization of 2-hydroxychalcone analogues of pyrazole 3a-3g using conc. HCl in acetic acid. The structures of the compounds 4a-4g were established by the combined use of (1)HNMR, IR and mass spectra. All the seven compounds were tested in vitro for their antibacterial activity against two Gram positive bacteria namely Staphylococcus aureus and Bacillus subtilis and two Gram negative bacteria Escherichia coli and Pseudomonas aeruginosa. The compounds 4b, 4c, 4e, 4f, 4g have displayed good antibacterial activity when compared with commercially available antibiotic, ciprofloxacin. These compounds also were screened for their antifungal activity against two ear pathogenic fungi, namely Aspergillus Niger and A. flavus. The compounds 4a, 4c, 4d, 4g exhibited good antifungal activity when compared with commercially available antifungal, fluconazole.
通过在乙酸中使用浓盐酸使吡唑3a - 3g的2 - 羟基查尔酮类似物环化，合成了七种新的2 - (3 - (4 - 芳基)-1 - 苯基-1H - 吡唑 - 4 - 基)苯并二氢吡喃 - 4 - 酮(4a - 4g)。通过联合使用(1)HNMR、红外光谱和质谱确定了化合物4a - 4g的结构。对所有七种化合物进行了体外测试，以检测它们对两种革兰氏阳性菌金黄色葡萄球菌和枯草芽孢杆菌以及两种革兰氏阴性菌大肠杆菌和铜绿假单胞菌的抗菌活性。与市售抗生素环丙沙星相比，化合物4b、4c、4e、4f、4g表现出良好的抗菌活性。还对这些化合物针对两种耳部致病真菌黑曲霉和黄曲霉的抗真菌活性进行了筛选。与市售抗真菌药氟康唑相比，化合物4a、4c、4d、4g表现出良好的抗真菌活性。
