Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists I: Discovery of CCKR1 selectivity in a previously CCKR2-selective lead series |
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| Authors: | Marna Pippel Brett D. Allison Victor K. Phuong Lina Li Magda F. Morton Clodagh Prendergast Xiaodong Wu Nigel P. Shankley Michael H. Rabinowitz |
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| Affiliation: | aJohnson & Johnson Pharmaceutical Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, United States |
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| 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. |
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