Amide bond replacements incorporated into CCK-B selective" dipeptoids"

…, DR Hill, DC Horwell, JC O'Toole…

文献索引：Fincham, Christopher I.; Higginbottom, Michael; Hill, David R.; Horwell, David C.; O'Toole, John C; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 8 p. 1472 - 1484

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被引用次数: 61

摘要

ICw= 125 nM, CCK-B IC,= 2580 nM, ratio= 21). The methyleneamino and hydroxyethylene replacements, which have been used elsewhere as transition-state inhibitors of enzymes, are poor mimics of the amide in these CCK-B receptor ligands. Some of the steric, lipophilic, and hydrogen bonding properties of amide replacements incorporated into the simple amide, N-methylacetamide, have been quantified with the aid of molecular modeling. ...