Romines, Karen R.; Freeman, George A.; Schaller, Lee T.; Cowan, Jill R.; Gonzales, Steve S.; Tidwell, Jeffrey H.; Andrews, Clarence W. III; Stammers, David K.; Hazen, Richard J.; Ferris, Robert G.; Short, Steven A.; Chan, Joseph H.; Boone, Lawrence R. published the artcile< Structure-Activity Relationship Studies of Novel Benzophenones Leading to the Discovery of a Potent, Next Generation HIV Nonnucleoside Reverse Transcriptase Inhibitor>, Synthetic Route of 22280-62-2, the main research area is AntiAIDS reverse transcriptase inhibitor benzophenone preparation structure activity HIV1; AIDS antiviral reverse transcriptase inhibitor benzophenone preparation HIV1.
Despite the progress of the past two decades, there is still considerable need for safe, efficacious drugs that target human immunodeficiency virus (HIV). This is particularly true for the growing number of patients infected with virus resistant to currently approved HIV drugs. Our high throughput screening effort identified a benzophenone template as a potential nonnucleoside reverse transcriptase inhibitor (NNRTI). This manuscript describes our extensive exploration of the benzophenone structure-activity relationships, which culminated in the identification of several compounds with very potent inhibition of both wild type and clin. relevant NNRTI-resistant mutant strains of HIV. These potent inhibitors include 70h (GW678248), which has in vitro antiviral assay IC50 values of 0.5 nM against wild-type HIV, 1 nM against the K103N mutant associated with clin. resistance to efavirenz, and 0.7 nM against the Y181C mutant associated with clin. resistance to nevirapine. Compound 70h has also demonstrated relatively low clearance in i.v. pharmacokinetic studies in three species, and it is the active component of a drug candidate which has progressed to phase 2 clin. studies.
Journal of Medicinal Chemistry published new progress about AIDS (disease). 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Synthetic Route of 22280-62-2.