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Article

Design, synthesis, X-ray studies, and biological evaluation of novel macrocyclic HIV-1 protease inhibitors involving the P1'-P2' ligands.

Bioorganic & medicinal chemistry letters - 1 Nov 2017

Ghosh Arun K, Sean Fyvie W, Brindisi Margherita, Steffey Melinda, Agniswamy Johnson, Wang Yuan-Fang, Aoki Manabu, Amano Masayuki, Weber Irene T, Mitsuya Hiroaki

Abstract excerpt

Design, synthesis, and evaluation of a new class of HIV-1 protease inhibitors containing diverse flexible macrocyclic P1'-P2' tethers are reported. Inhibitor 5a with a pyrrolidinone-derived macrocycle exhibited favorable enzyme inhibitory and antiviral activity (Ki=13.2nM, IC50=22nM). Further incorporation of heteroatoms in the macrocyclic skeleton provided macrocyclic inhibitors 5m and 5o. These compounds showed...

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Identifiers

PMID: 28958624
DOI: 10.1016/j.bmcl.2017.09.003
PMCID: PMC5647257

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 5 Sept 2026. Manifest publication-graph-cohort-2026-09-05.1.

Source receipt: pubmed, retrieved 5 Sept 2026.

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