Novel 2-chloro-8-arylthiomethyldipyridodiazepinone derivatives with activity against HIV-1 reverse transcriptase

Nisachon Khunnawutmanotham; Nitirat Chimnoi; Patchareenart Saparpakorn; Pornpan Pungpo; Suda Louisirirotchanakul; Supa Hannongbua; Supanna Techasakul

doi:10.3390/12020218

Novel 2-chloro-8-arylthiomethyldipyridodiazepinone derivatives with activity against HIV-1 reverse transcriptase

Molecules. 2007 Feb 20;12(2):218-30. doi: 10.3390/12020218.

Authors

Nisachon Khunnawutmanotham¹, Nitirat Chimnoi, Patchareenart Saparpakorn, Pornpan Pungpo, Suda Louisirirotchanakul, Supa Hannongbua, Supanna Techasakul

Affiliation

¹ Chulabhorn Research Institute, Vibhavadee-Rangsit Highway, Bangkok 10210, Thailand. [email protected]

Abstract

Based on the molecular modeling analysis against Y181C HIV-1 RT, dipyridodiazepinone derivatives containing an unsubstituted lactam nitrogen and 2-chloro-8-arylthiomethyl were synthesized via an efficient route. Some of them were evaluated for their antiviral activity against HIV-1 RT subtype E and were found to exhibit virustatic activity comparable to some clinically used therapeutic agents.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anti-HIV Agents / chemical synthesis
Anti-HIV Agents / chemistry*
Anti-HIV Agents / pharmacology*
Azepines / chemical synthesis
Azepines / chemistry*
Azepines / pharmacology*
Cells, Cultured
HIV Reverse Transcriptase / antagonists & inhibitors*
HIV-1 / enzymology*
Humans
Models, Molecular
Molecular Structure
Structure-Activity Relationship
Virus Replication / drug effects

Substances

Anti-HIV Agents
Azepines
HIV Reverse Transcriptase