872703-69-0Relevant articles and documents
Microwave-accelerated synthesis of P1′-extended HIV-1 protease inhibitors encompassing a tertiary alcohol in the transition-state mimicking scaffold
Ekegren, Jenny K.,Ginman, Nina,Johansson, ?sa,Wallberg, Hans,Larhed, Mats,Samuelsson, Bertil,Unge, Torsten,Hallberg, Anders
, p. 1828 - 1832 (2007/10/03)
Two series of P1′-extended HIV-1 protease inhibitors comprising a tertiary alcohol in the transition-state mimic exhibiting Ki values ranging from 2.1 to 93 nM have been synthesized. Microwave-accelerated palladium-catalyzed cross-couplings were utilized to rapidly optimize the P1′ side chain. High cellular antiviral potencies were encountered when the P1′ benzyl group was elongated with a 3- or 4-pyridyl substituent (EC50 = 0.18-0.22 μM). X-ray crystallographic data were obtained for three inhibitors cocrystallized with the enzyme.
A new class of HIV-1 protease inhibitors containing a tertiary alcohol in the transition-state mimicking scaffold
Ekegren, Jenny K.,Unge, Torsten,Safa, Mayada Zreik,Wallberg, Hans,Samuelsson, Bertil,Hallberg, Anders
, p. 8098 - 8102 (2007/10/03)
Novel HIV-1 protease inhibitors encompassing a tertiary alcohol as part of the transition-state mimicking unit have been synthesized. Variation of the P1′-P3′ residues and alteration of the tertiary alcohol absolute stereochemistry a