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Article

A new class of HIV-1 protease inhibitors containing a tertiary alcohol in the transition-state mimicking scaffold.

Journal of medicinal chemistry - 15 Dec 2005

Ekegren Jenny K, Unge Torsten, Safa Mayada Zreik, Wallberg Hans, Samuelsson Bertil, Hallberg Anders

Abstract excerpt

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...

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Source

Identifiers

PMID: 16335934
DOI: 10.1021/jm050790t

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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