CCR2B receptor antagonists: conversion of a weak HTS hit to a potent lead compound

A weak HTS hit at the CCR2B receptor has been converted into a potent antagonist by array SAR studies. Selectivity over the closely related CCR5 receptor is also achieved.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-08, Vol.10 (16), p.1803-1806
Hauptverfasser:	Forbes, Ian T, Cooper, David G, Dodds, Emma K, Hickey, Deirdre M.B, Ife, Robert J, Meeson, Malcolm, Stockley, Martin, Berkhout, Theo A, Gohil, Jayneeta, Groot, Pieter H.E, Moores, Kitty
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemical synthesis Amides - chemistry Amides - metabolism Amides - pharmacology Biological and medical sciences Chemokine CCL2 - chemistry Chemokine CCL2 - metabolism Chemotaxis, Leukocyte - drug effects Humans Indoles - chemical synthesis Indoles - chemistry Indoles - metabolism Indoles - pharmacology Kinetics Ligands Medical sciences Miscellaneous Molecular Structure Monocytes - drug effects Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - chemistry Piperidines - metabolism Piperidines - pharmacology Receptors, CCR2 Receptors, CCR5 - metabolism Receptors, Chemokine - antagonists & inhibitors Receptors, Chemokine - chemistry Receptors, Chemokine - metabolism Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	A weak HTS hit at the CCR2B receptor has been converted into a potent antagonist by array SAR studies. Selectivity over the closely related CCR5 receptor is also achieved.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00347-4