European Journal of Medicinal Chemistry p. 202 - 212 (2013)
Update date:2022-08-03
Topics:
Velthuisen, Emile J.
Baughman, Todd M.
Johns, Brian A.
Temelkoff, David P.
Weatherhead, Jason G.
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.
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