Synthesis and different biological activities of novel benzoxazoles

Temiz-Arpaci, O. and Eylem Cifcioglu Goztepe, B. and Kaynak-Onurdag, Fatma and Ozgen, Selda and Senol, Fatma and Erdogan Orhan, I. (2013) Synthesis and different biological activities of novel benzoxazoles. Acta Biologica Hungarica, 64 (2). pp. 249-261. ISSN 0236-5383

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Abstract

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.

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