Ontology highlight
ABSTRACT:
SUBMITTER: Ghosh AK
PROVIDER: S-EPMC4133278 | biostudies-literature | 2014 Sep
REPOSITORIES: biostudies-literature
Ghosh Arun K AK Schiltz Gary E GE Rusere Linah N LN Osswald Heather L HL Walters D Eric DE Amano Masayuki M Mitsuya Hiroaki H
Organic & biomolecular chemistry 20140901 35
A series of potent macrocyclic HIV-1 protease inhibitors have been designed and synthesized. The compounds incorporated 16- to 19-membered macrocyclic rings between a nelfinavir-like P2 ligand and a tyrosine side chain containing a hydroxyethylamine sulfonamide isostere. All cyclic inhibitors are more potent than their corresponding acyclic counterparts. Saturated derivatives showed slight reduction of potency compared to the respective unsaturated derivatives. Compound containing a 16-membered ...[more]