Ersan S, Nacak S, Berkem R, Ozden T
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, Ankara, Turkey.
Arzneimittelforschung. 1997 Aug;47(8):963-5.
New 2-[(alpha-methylbenzylidene)hydrazino]benzoxazole derivatives have been synthesized by reacting ortho or para substituted acetophenones with 2-hydrazinobenzoxazole in ethanol. The structures of the synthesized compounds were confirmed by microanalysis, IR and NMR spectral data. Antimicrobial activities of the compounds were investigated by the microdilution susceptibility test in Mueller-Hinton broth and Sabouraud liquid medium. Test organisms: Staphylococcus aureus ATCC 29213 and Enterococcus faecalis ATCC 29212 as Gram (+) bacteria, Escherichia coli ATCC 25922 and Pseudomonas aeruginosa, ATCC 27853 as Gram (-) bacteria, and Candida albicans, Candida stellatoidea, Candida parapsilosis and Candida pseudotropicalis as yeasts. Among the compounds tested 2-[(alpha-methyl-4-chlorobenzylidene)hydrazino]benzoxazole (compounds 4) and 2-[(alpha-methyl-4-nitrobenzylidene)hydrazino]benzoxazole (compound 8) showed the most favorable activity.
通过使邻位或对位取代的苯乙酮与2-肼基苯并恶唑在乙醇中反应，合成了新型的2-[(α-甲基亚苄基)肼基]苯并恶唑衍生物。通过微量分析、红外光谱和核磁共振光谱数据确认了合成化合物的结构。通过在 Mueller-Hinton 肉汤和沙氏液体培养基中进行微量稀释药敏试验，研究了这些化合物的抗菌活性。测试菌株：金黄色葡萄球菌 ATCC 29213 和粪肠球菌 ATCC 29212 作为革兰氏阳性菌，大肠埃希菌 ATCC 25922 和铜绿假单胞菌 ATCC 27853 作为革兰氏阴性菌，以及白色念珠菌、星状念珠菌、近平滑念珠菌和伪热带念珠菌作为酵母菌。在所测试的化合物中，2-[(α-甲基-4-氯亚苄基)肼基]苯并恶唑（化合物4）和2-[(α-甲基-4-硝基亚苄基)肼基]苯并恶唑（化合物8）表现出最有利的活性。
