Temiz-Arpaci O, Eylem Cifcioglu Goztepe B, Kaynak-Onurdag Fatma, Ozgen Selda, Senol Fatma Sezer, Erdogan Orhan I
Department of Pharmaceutical Chemistry, Ankara University, Ankara, Turkey.
Acta Biol Hung. 2013 Jun;64(2):249-61. doi: 10.1556/ABiol.64.2013.2.10.
A series of 2-[4-(4-substitutedbenzamido/phenylacetamido/butanamido)phenyl]-5-ethylsulphonyl-benzoxazole derivatives were synthesized and biologically evaluated as possible antimicrobial agents and inhibitors of tyrosinase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). The results demonstrated that the synthesized compounds exhibited a broad spectrum of activity with minimum inhibitory concentration (MIC) values of 128-16 μg/ml against some Gram-positive, Gram-negative bacteria as well as Candida albicans and C. krusei. The compound 10 displayed higher activity in this series against methicilline resistant Staphylococcus aureus (MRSA) with a MIC value of 16 μg/ml than the compared control drugs ampicillin and ceftriaxone. Compound 14 showed moderate tyrosinase inhibition, however, none of the compounds showed effect as inhibitor of AChE and BChE.
合成了一系列2-[4-(4-取代苯甲酰胺基/苯乙酰氨基/丁酰胺基)苯基]-5-乙基磺酰基苯并恶唑衍生物，并作为可能的抗菌剂以及酪氨酸酶、乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BChE）的抑制剂进行了生物学评价。结果表明，合成的化合物表现出广谱活性，对一些革兰氏阳性菌、革兰氏阴性菌以及白色念珠菌和克柔念珠菌的最低抑菌浓度（MIC）值为128 - 16μg/ml。化合物10在该系列中对耐甲氧西林金黄色葡萄球菌（MRSA）表现出更高的活性，MIC值为16μg/ml，高于对照药物氨苄西林和头孢曲松。化合物14表现出中等程度的酪氨酸酶抑制作用，然而，没有一种化合物表现出作为AChE和BChE抑制剂的作用。
