Discovery of potent HIV-1 protease inhibitors incorporating sulfoximine functionality
Based on the unique property of sulfoximine and the homodimeric C2 structural symmetry of HIV-1 protease, a novel class of sulfoximine-based pseudosymmetric HIV-1 protease inhibitors was designed and synthesized. The sulfoximine moiety was demonstrated to be important for HIV-1 protease inhibitor potency. The most active stereoisomer (2S,2′S) displays a potency of 2.5 nM (IC50) against HIV-1 protease and an anti-HIV-1 activity of 408 nM (IC50). A possible mode of action is proposed.
Lu, Ding,Vince, Robert
p. 5614 - 5619
(2008/03/13)
HIV protease inhibitors
Compounds of the formula (I): Wherein R1, R2, X and N are as defined in the specification; E is N, CH; A1 and A" are terminal groups as defined in the specification. The compounds have utility as HIV-I protease inhibitors.
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Page/Page column 54
(2008/06/13)
A new class of HIV-1 protease inhibitors containing a tertiary alcohol in the transition-state mimicking scaffold
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
Ekegren, Jenny K.,Unge, Torsten,Safa, Mayada Zreik,Wallberg, Hans,Samuelsson, Bertil,Hallberg, Anders
p. 8098 - 8102
(2007/10/03)
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