Structural highlights
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
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 afforded 10 inhibitors. High potencies for the compounds with (S)-configuration at the carbon carrying the tertiary hydroxyl group were achieved with Ki values down to 2.4 nM. X-ray crystallographic data for a representative compound in complex with HIV-1 protease are presented.
A new class of HIV-1 protease inhibitors containing a tertiary alcohol in the transition-state mimicking scaffold.,Ekegren JK, Unge T, Safa MZ, Wallberg H, Samuelsson B, Hallberg A J Med Chem. 2005 Dec 15;48(25):8098-102. PMID:16335934[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Ekegren JK, Unge T, Safa MZ, Wallberg H, Samuelsson B, Hallberg A. A new class of HIV-1 protease inhibitors containing a tertiary alcohol in the transition-state mimicking scaffold. J Med Chem. 2005 Dec 15;48(25):8098-102. PMID:16335934 doi:10.1021/jm050790t
