189391-01-3Relevant academic research and scientific papers
8-arylalkyl- and 8-arylheteroalkyl-5,11-dihydro-6H-dipyrido?3,2-B:2',3'-e!?1!diazepines and their use in the treatment of HIV-1 infection
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, (2008/06/13)
Disclosed are novel 8-arylalkyl-5,11-dihydro-6H-dipyrido?3,2-b:2',3'-e!?1,4!diazepines. These are useful in the treatment of HIV-1 infection.
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 7. 8- Arylethyldipyridodiazepinones as potent broad-spectrum inhibitors of wild- type and mutant enzymes
Klunder, Janice M.,Hoermann, MaryAnn,Cywin, Charles L.,David, Eva,Brickwood, Janice R.,Schwartz, Racheline,Barringer, Kevin J.,Pauletti, Daniel,Shih, Cheng-Kon,Erickson, David A.,Sorge, Christopher L.,Joseph, David P.,Hattox, Susan E.,Adams, Julian,Grob, Peter M.
, p. 2960 - 2971 (2007/10/03)
Like other nonnucleoside inhibitors of HIV-1 reverse transcriptase, the dipyridodiazepinone nevirapine (Viramune, 1) selects for drug resistant variants of HIV-1, both in cell culture and in patients. In particular, the mutation of residue 181 from tyrosine to cysteine (Y181C) is associated with resistance to most reported nonnucleoside inhibitors. Introduction of an arylethyl substituent at the 8-position of the tricyclic dipyridodiazepinone skeleton confers enhanced potency against Y181C RT. Several analogues of this series display good broad spectrum potency against a panel of mutant enzymes.
8-Arylalkyl- and 8-arylheteroalkyl-5, 11-dihydro-6H-dipyrido-[3,2-b:2', 3'-e][1,4]diazepines and their use in the prevention or treatment of HIV infection
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, (2008/06/13)
The invention relates to novel 8-arylalkyl-5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepines of general formula 1 which are useful in the prevention or treatment of HIV infection.
