Novel 2-Chloro-8-arylthiomethyldipyridodiazepinone Derivatives with Activity against HIV-1 Reverse Transcriptase

Abstract

Based on the molecular modeling analysis against Y181CHIV-1 RT, dipyridodiazepinone derivatives containing an unsubstituted lactamnitrogen and 2-chloro-8-arylthiomethyl were synthesized via an efficientroute. Some of them were evaluated for their antiviral activity against HIV-1RT subtype E and were found to exhibit virustatic activity comparable to some clinically usedtherapeutic agents.

Keywords

• Dipyridodiazepinone
• HIV-1 RT
• antiviral activity