SAR studies of 1,5-diarylpyrazole-based CCK1 receptor antagonists

A high throughput screening campaign revealed compound 1 as a potent antagonist of the human CCK(1) receptor. Here, we report the syntheses and SAR studies of 1,5-diarylpyrazole analogs with various structural modifications of the alkane side chain of the molecule. The difference in affinity between...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-12, Vol.17 (23), p.6493-6498
Hauptverfasser:	GOMEZ, Laurent, HACK, Michael D, MCCLURE, Kelly, SEHON, Clark, LIMING HUANG, MORTON, Magda, LINA LI, BARRETT, Terrance D, SHANKLEY, Nigel, BREITENBUCHER, J. Guy
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Humans Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Pyrazoles - chemistry Pyrazoles - pharmacology Rats Receptor, Cholecystokinin A - antagonists & inhibitors Receptor, Cholecystokinin A - physiology Structure-Activity Relationship
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Zusammenfassung:	A high throughput screening campaign revealed compound 1 as a potent antagonist of the human CCK(1) receptor. Here, we report the syntheses and SAR studies of 1,5-diarylpyrazole analogs with various structural modifications of the alkane side chain of the molecule. The difference in affinity between the two enantiomers for the CCK(1) receptor and the flexible nature of the linker led to the design of constrained analogs with increased potency.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2007.09.093