Ontology highlight
ABSTRACT:
SUBMITTER: Curreli F
PROVIDER: S-EPMC4676410 | biostudies-literature | 2015 Sep
REPOSITORIES: biostudies-literature
Curreli Francesca F Kwon Young Do YD Zhang Hongtao H Scacalossi Daniel D Belov Dmitry S DS Tikhonov Artur A AA Andreev Ivan A IA Altieri Andrea A Kurkin Alexander V AV Kwong Peter D PD Debnath Asim K AK
Journal of medicinal chemistry 20150828 17
Earlier we reported the discovery and design of NBD-556 and their analogs which demonstrated their potential as HIV-1 entry inhibitors. However, progress in developing these inhibitors has been stymied by their CD4-agonist properties, an unfavorable trait for use as drug. Here, we demonstrate the successful conversion of a full CD4-agonist (NBD-556) through a partial CD4-agonist (NBD-09027), to a full CD4-antagonist (NBD-11021) by structure-based modification of the critical oxalamide midregion, ...[more]