Identification and optimization of anthranilic sulfonamides as novel, selective cholecystokinin-2 receptor antagonists

…, X Wu, H Venkatesan, M Pippel, C Woods…

Index: Allison, Brett D.; Phuong, Victor K.; McAtee, Laura C.; Rosen, Mark; Morton, Magda; Prendergas, Clodagh; Barrett, Terry; Lagaud, Guy; Freedman, Jamie; Li, Na; Wu, Xiaodong; Venkatesan, Hariharan; Pippel, Marna; Woods, Craig; Rizzolio, Michele C.; Hack, Michael; Hoey, Kenway; Deng, Xiaohu; King, Christopher; Shankley, Nigel P.; Rabinowitz, Michael H. Journal of Medicinal Chemistry, 2006 , vol. 49, # 21 p. 6371 - 6390

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Citation Number: 31

Abstract

A high throughput screening approach to the identification of selective cholecystokinin-2 receptor (CCK-2R) ligands resulted in the discovery of a novel series of antagonists, represented by 1-[2-[(2, 1, 3-benzothiadiazol-4-ylsulfonyl) amino]-5-chlorobenzoyl]- piperidine (1; CCK-2R, p KI= 6.4). Preliminary exploration of the structure-activity relationships around the anthranilic ring and the amide and sulfonamide moieties led to a ...