发现新型磺酰胺-吡唑并哌啶系列作为有效和高效的γ-分泌酶抑制剂。
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors.
机构信息
Department of Medicinal Chemistry, Elan Pharmaceuticals, 800 Gateway Boulevard, South San Francisco, CA 94080, United States.
出版信息
Bioorg Med Chem Lett. 2010 Apr 1;20(7):2195-9. doi: 10.1016/j.bmcl.2010.02.039. Epub 2010 Feb 13.
PMID:20207136
Abstract
Discovery of a series of pyrazolopiperidine sulfonamide based gamma-secretase inhibitors and its SAR evolution is described. Significant increases in APP potency on the pyrazolopiperidine scaffold over the original N-bicyclic sulfonamide scaffold were achieved and this potency increase translated in an improved in vivo efficacy.
摘要
本文描述了一系列吡唑并哌啶磺酰胺类γ-分泌酶抑制剂的发现及其 SAR 进化。在吡唑并哌啶骨架上相对于原始的 N-双环磺酰胺骨架，显著提高了 APP 的效力，并且这种效力的提高转化为改善的体内疗效。
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