Synthesis and different biological activities of novel benzoxazoles

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.

Synthesis and antimicrobial evaluation of some novel sulfonylamido-benzoxazoles

“…In the last years we described the synthesis of different derivatives of some 2,5-di substituted benzoxazoles and the results of assays on their in vitro antimicrobial activity against some Gram-positive, Gram-negative bacteria and fungus Candida albicans [1][2][15][16][17]. In the present study, we report a new series of 2-(p-sub stituted phenyl)-5-[(4-substituted phenyl) sulfonylamido]-benzoxazoles.…”

Synthesis, vibrational spectroscopic investigations, molecular docking, antibacterial and antimicrobial studies of 5-ethylsulphonyl-2-(p-aminophenyl)benzoxazole

“…The synthesis of the 5-ethylsulphonyl-2-(p-aminophenyl)benzoxazole (1) was obtained by heating p-aminobenzoic acid with 4-ethylsulphonyl-2-aminophenol in PPA (polyphosphoric acid) as the cyclodehydration reagent in a one step procedure [15]. 2.…”

“…The residue was boiled with 200 mg charcoal in ethanol and filtered. After the evaporation of solvent in vacuo, the crude product was obtained and recrystallized from ethanol-water mixture and compound 1 was dried in vacuo [15].…”

Novel pyranopyrazole derivatives comprising a benzoxazole core as antimicrobial inhibitors: Design, synthesis, microbial resistance and machine aided results

“…Benzoheterocycles like benzoxazoles are prominent heterocycles. Because in the medicinal chemistry point of view these compounds exhibited different types of medicinal properties [13][14][15]. Moreover, almost ten efficient drugs in the top two hundred medical products are benzoxazole related products [16].…”