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.
[Hargrave, Karl D.; Proudfoot, John R.; Grozinger, Karl G.; Cullen, Ernest; Kapadia, Suresh R.; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 7 p. 2231 - 2241]
[Hargrave, Karl D.; Proudfoot, John R.; Grozinger, Karl G.; Cullen, Ernest; Kapadia, Suresh R.; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 7 p. 2231 - 2241]