- Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists I: discovery of CCKR1 selectivity in a previously CCKR2-selective lead series.
Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists I: discovery of CCKR1 selectivity in a previously CCKR2-selective lead series.
Bioorganic & medicinal chemistry letters (2009-10-09)
Marna Pippel, Brett D Allison, Victor K Phuong, Lina Li, Magda F Morton, Clodagh Prendergast, Xiaodong Wu, Nigel P Shankley, Michael H Rabinowitz
PMID19811913
摘要
A series of CCK2R-selective anthranilic amides is shown to derive CCK1R affinity via selective substitution of the amide side chain. Thus, extending the length of the original benzamide side chain by a single methylene unit imparts CCK1R affinity to the series, and further fine tuning of the affinity results in CCK1R selectivity of greater than 100-fold.
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