1033464-75-3Relevant academic research and scientific papers
Discovery of potent cholecystokinin-2 receptor antagonists: Elucidation of key pharmacophore elements by X-ray crystallographic and NMR conformational analysis
Rosen, Mark D.,Hack, Michael D.,Allison, Brett D.,Phuong, Victor K.,Woods, Craig R.,Morton, Magda F.,Prendergast, Clodagh E.,Barrett, Terrance D.,Schubert, Carsten,Li, Lina,Wu, Xiaodong,Wu, Jiejun,Freedman, Jamie M.,Shankley, Nigel P.,Rabinowitz, Michael H.
, p. 3917 - 3925 (2008/12/20)
A novel series of cholecystokinin-2 receptor (CCK-2R) antagonists has been identified, as exemplified by anthranilic sulfonamide 1 (pKi = 7.6). Pharmacokinetic and stability studies indicated that this series of compounds suffered from metabolic degradation, and that both the benzothiadiazole and piperidine rings were rapidly oxidized by liver enzymes. A combination of synthesis, computational methods, 1H NMR conformational studies, and X-ray crystallographic analyses were applied to elucidate key pharmacophore elements, and to discover analogs with improved pharmacokinetic profiles, and high receptor binding affinity and selectivity.
ARYL SULFONAMIDE COMPOUNDS AS MODULATORS OF THE CCK2 RECEPTOR
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Page/Page column 21, (2008/12/04)
Certain aryl sulfonamide compounds are CCK2 receptor modulators useful in the treatment of CCK2 receptor-mediated diseases.
