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1. Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists I: Discovery of CCKR1 selectivity in a previously CCKR2-selective lead series

Author

Pippel, Marna, Allison, Brett D., Phuong, Victor K., Li, Lina, Morton, Magda F., Prendergast, Clodagh, Wu, Xiaodong, Shankley, Nigel P., and Rabinowitz, Michael H.

Subjects
*SULFONAMIDES, *OXAZOLES, *DRUG development, *CHOLECYSTOKININ, *BENZAMIDE, *HORMONE antagonists, *THERAPEUTICS
Abstract

Abstract: 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. [Copyright &y& Elsevier]

Published
2009
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