152438-62-5Relevant articles and documents
Synthesis and pharmacokinetic profile of highly deuterated brecanavir analogs
Velthuisen, Emile J.,Baughman, Todd M.,Johns, Brian A.,Temelkoff, David P.,Weatherhead, Jason G.
, p. 202 - 212 (2013/07/27)
Several highly deuterated analogs of the HIV-1 protease inhibitor brecanavir have been prepared to study the effect of deuterium upon metabolic stability. The sites for deuterium incorporation were initially chosen to maximize the potential for a kinetic isotope effect; locations where C-H bond breaking is the rate limiting step. The analogs have been profiled in both in vitro and in vivo pharmacokinetic studies and the result will be described herein.
Novel P1 chain-extended HIV protease inhibitors possessing potent anti-HIV activity and remarkable inverse antiviral resistance profiles
Miller, John F.,Brieger, Michael,Furfine, Eric S.,Hazen, Richard J.,Kaldor, Istvan,Reynolds, David,Sherrill, Ronald G.,Spaltenstein, Andrew
, p. 3496 - 3500 (2007/10/03)
A novel series of tyrosine-derived HIV protease inhibitors was synthesized and evaluated for in vitro antiviral activity against wild-type virus and two protease inhibitor-resistant viruses. All of the compounds had wild-type antiviral activities that were similar to or greater than several currently marketed HIV protease inhibitors. In addition, a number of compounds in this series were more potent against the drug-resistant mutant viruses than they were against wild-type virus.
A practical method for the preparation of α'-chloroketones of N-carbanaate protected-α-aminoacids
Chen, Ping,Cheng, Peter T. W.,Spergel, Steven H.,Zahler, Robert,Wang, Xuebao,Thottathil, John,Barrish, Joel C.,Polniaszek, Richard P.
, p. 3175 - 3178 (2007/10/03)
A practical method for the preparation of α-N-BOC-epoxides from protected amino acid esters based on the Kowalski homologation reaction is described. This procedure can be readily performed on a large scale without the use of hazardous reagents and has allowed preparation of epoxides 3 in multi-kilogram quantities.