Journal of Medicinal Chemistry p. 1828 - 1832 (2006)
Update date:2022-08-04
Topics:
Ekegren, Jenny K.
Ginman, Nina
Johansson, ?sa
Wallberg, Hans
Larhed, Mats
Samuelsson, Bertil
Unge, Torsten
Hallberg, Anders
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.
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