17 research outputs found
Synthesis and different biological activities of novel benzoxazoles
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
A study on the antioxidant activities of some new benzazole derivatives
The
in vitro
antioxidant properties of some new benzazole derivatives (
1–10
) such as benzoxazoles, ben-
zimidazoles, and benzothiazoles were determined by their effects on the rat liver microsomal NADPH-
dependent lipid peroxidation (LP) level, the scavenging of superoxide anion and the stable radical 2,2-
diphenyl-1-picrylhydrazyl (DPPH). Compounds
1
,
2
,
4
and
6
, showed potent scavenging effect on super-
oxide radical at 10
–3
M. Compound
8,
5-nitro-2-(phenoxymethyl)benzimidazole, strongly inhibited lipid
peroxidation at 10
–3
M concentration