Department of Chemistry, Faculty of Science, King Abdulaziz University , Jeddah , Saudi Arabia.
J Enzyme Inhib Med Chem. 2013 Oct;28(5):926-35. doi: 10.3109/14756366.2012.694880. Epub 2012 Jul 18.
The synthesis, in vitro antimicrobial activities of some novel hydroxy pyridines supported with various pharmacophores is described. Twenty-six out of the tested 58 compounds exhibited variable inhibitory effects on the growth of the tested Gram positive and Gram negative bacteria. The tested compounds revealed better activity against the Gram positive rather than the Gram negative strains. The synthesized hydroxypyridones have shown very significant inhibitory effect against Staphylococcus aureus and Bacillus subtilis. Twelve compounds namely; 5d, 5f, 6a, 6b, 8b, 18b, 18c, 19c, 21d, 22b, 22d and 23d were able to produce appreciable growth inhibitory activity against Candida albicans when compared to Clotrimazole. Among these, 22d proved to be the most potent antifungal agent.
描述了一些新型带有不同药效团的羟基吡啶的合成及其体外抗菌活性。在所测试的 58 种化合物中，有 26 种对测试的革兰氏阳性菌和革兰氏阴性菌的生长表现出不同程度的抑制作用。测试的化合物对革兰氏阳性菌的活性优于革兰氏阴性菌。所合成的羟基吡啶酮对金黄色葡萄球菌和枯草芽孢杆菌表现出非常显著的抑制作用。当与克霉唑相比时，有 12 种化合物，即 5d、5f、6a、6b、8b、18b、18c、19c、21d、22b、22d 和 23d，能够对白色念珠菌产生明显的生长抑制活性。其中，22d 被证明是最有效的抗真菌剂。
