Synthesis and anti HIV-1 activity of new thiadiazepindioxides

✍ Scribed by Danilo Giannotti; Giovanni Viti; Rossano Nannicini; Vittorio Pestellini; Daniela Bellarosa

• Book ID: 103982994
• Publisher: Elsevier Science
• Year: 1995
• Tongue: English
• Weight: 270 KB
• Volume: 5
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/0960-894x(95)00257-t

✦ Synopsis

New pyridobenzo-and dipyridothiadiazepindioxides 3-5 and two isomers 13-14 were synthetized and their anti HIV-1 activity and the cytotoxicity were evaluated in vitro. A good antiviral activity was shown by pyridobenzothiadiazepindioxides 4, compound 4a being the best.

The human immunodeficiency virus type 1 (HIV-1) reverse transcriptase is an important target for the development of potent and effective drugs against the acquired immunodeficiency syndrome (AIDS) l, since the process of reverse transcription is an essential step in the HIV-1 life cycle. Recently several non-nucleoside reverse transcriptase inhibitors (NNRTIs) such as Nevirapine, TIBO, 0t-APA, Pyridinones and Bis(heteroaryl)piperazines have been introduced in clinical trials 2.