Synthesis and HIV-1 reverse transcriptase inhibitor activity of some 2,5,6-substituted benzoxazole, benzimidazole, benzothiazole and oxazolo (4,5-b)pyridine derivatives

Akbay A., Oren İ., ARPACI Ö., Aki-Sener E., Yalcin I.

Arzneimittel-Forschung/Drug Research, vol.53, no.4, pp.266-271, 2003 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 53 Issue: 4
  • Publication Date: 2003
  • Doi Number: 10.1055/s-0031-1297107
  • Journal Name: Arzneimittel-Forschung/Drug Research
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.266-271
  • Keywords: antiviral drugs, benzimidazoles, benzothiazoles, HIV-1 reverse transcriptase, enzyme inhibitors, oxazolo(4,5-b)pyridines, MICROBIOLOGICAL ACTIVITY, L-696,229, ANALOGS
  • Ankara University Affiliated: Yes

Abstract

In this study, the synthesis of some benzoxazoles and their analogues were described and their antiviral activities were studied together with the previously synthesized 2,5,6-trisubstituted benzoxazole, benzothiazole, benzimidazole and oxazolo(4,5-b)pyridine derivatives. The reverse transcriptase (RT) inhibitory activity of these compounds was determined using a commercial kit and assay system which utilizes the scintillation proximity assay principle. The results are concentration at which the compound inhibits RT activity by 50%). The compounds inhibited the in vitro binding of thymidine to the RT enzyme exhibiting IC50 values between 6.3 × 105 μmol/l-0.34 μmol/l and their activities were compared to some standard drugs such as 3′-azido-2′,3′-dideoxythymidine triphosphate and dideoxythymidine triphosphate.