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

…, L Li, TD Barrett, N Shankley, JG Breitenbucher

Index: Gomez, Laurent; Hack, Michael D.; McClure, Kelly; Sehon, Clark; Huang, Liming; Morton, Magda; Li, Lina; Barrett, Terrance D.; Shankley, Nigel; Breitenbucher, J. Guy Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 23 p. 6493 - 6498

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Citation Number: 18

Abstract

A high throughput screening campaign revealed compound 1 as a potent antagonist of the human CCK1 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 CCK1 receptor and the flexible nature of the linker led to the design of constrained analogs with increased ...