Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection

D Kim; L Wang; C G Caldwell; P Chen; P E Finke; B Oates; M MacCoss; S G Mills; L Malkowitz; S L Gould; J A DeMartino; M S Springer; D Hazuda; M Miller; J Kessler; R Danzeisen; G Carver; A Carella; K Holmes; J Lineberger; W A Schleif; E A Emini

doi:10.1016/s0960-894x(01)00654-0

Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection

Bioorg Med Chem Lett. 2001 Dec 17;11(24):3099-102. doi: 10.1016/s0960-894x(01)00654-0.

Authors

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, RY 121-240, PO Box 2000, Rahway, NJ 07065, USA. dooseop_kim@merck.com

PMID: 11720851
DOI: 10.1016/s0960-894x(01)00654-0

Abstract

A series of hydantoin derivatives has been discovered as highly potent nonpeptide antagonists for the human CCR5 receptor. The synthesis, SAR, and biological profiles of this class of antagonists are described.

MeSH terms

Anti-HIV Agents / chemistry
Anti-HIV Agents / pharmacology
Anti-HIV Agents / therapeutic use*
CCR5 Receptor Antagonists*
HIV Infections / drug therapy*
HIV-1 / isolation & purification
Humans
Hydantoins / chemistry
Hydantoins / pharmacology
Hydantoins / therapeutic use*

Substances

Anti-HIV Agents
CCR5 Receptor Antagonists
Hydantoins