SYNTHESIS AND DIFFERENT BIOLOGICAL ACTIVITIES OF NOVEL BENZOXAZOLES

ARPACI Ö., Goztepe B. E. C., Kaynak-Onurdag F., Ozgen S., ŞENOL DENİZ F. S., ERDOĞAN ORHAN İ.

ACTA BIOLOGICA HUNGARICA, vol.64, no.2, pp.249-261, 2013 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 64 Issue: 2
  • Publication Date: 2013
  • Doi Number: 10.1556/abiol.64.2013.2.10
  • Journal Name: ACTA BIOLOGICA HUNGARICA
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.249-261
  • Keywords: Benzoxazoles, antibacterial activity, antifungal activity, enzyme inhibition, synthesis, TYROSINASE INHIBITORS, ANTICANCER, DERIVATIVES, ANALOGS, ACETYLCHOLINESTERASE, BENZIMIDAZOLES
  • Ankara University Affiliated: Yes

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 mu g/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 mu g/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.