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

Molecules

Nisachon Khunnawutmanotham²  Nitirat Chimnoi²  Patchareenart Saparpakorn³  Pornpan Pungpo⁴  Suda Louisirirotchanakul¹  Supa Hannongbua³ 

[1] Department of Microbiology, Siriraj Hospital, Mahidol University, Bangkok 10700, Thailand; E-mail:;Chulabhorn Research Institute, Vibhavadee-Rangsit Highway, Bangkok 10210, Thailand; E-mails:;Department of Chemistry, Faculty of Science, Kasetsart University, Bangkok 10903, Thailand; E-mails:;Department of Chemistry, Faculty of Science, Ubonratchathani University, Ubonratchathani 34190, Thailand; E-mail:

关键词: Dipyridodiazepinone;    HIV-1 RT;    antiviral activity;   

DOI  :  10.3390/12020218

来源: mdpi

【 摘 要 】

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.

【 授权许可】

Unknown   
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