Synthesis and different biological activities of novel benzoxazoles

Temiz-Arpaci O., Goztepe B. E. C., Kaynak-Onurdag F., Ozgen S., ŞENOL DENİZ F. S., Orhan İ.

Acta Biologica Hungarica, cilt.64, sa.2, ss.249-261, 2013 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 64 Sayı: 2
  • Basım Tarihi: 2013
  • Doi Numarası: 10.1556/abiol.64.2013.2.10
  • Dergi Adı: Acta Biologica Hungarica
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.249-261
  • Anahtar Kelimeler: Benzoxazoles, antibacterial activity, antifungal activity, enzyme inhibition, synthesis, TYROSINASE INHIBITORS, ANTICANCER, DERIVATIVES, ANALOGS, ACETYLCHOLINESTERASE, BENZIMIDAZOLES
  • Lokman Hekim Üniversitesi Adresli: Hayır

Özet

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. © 2013 Akadémiai Kiadó, Budapest.