磺酰胺-吡唑γ-分泌酶抑制剂的发现。

Discovery of sulfonamide-pyrazole gamma-secretase inhibitors.

机构信息

Elan Pharmaceuticals, 800 Gateway Blvd., South San Francisco, CA 94080, United States.

出版信息

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2148-50. doi: 10.1016/j.bmcl.2010.02.050. Epub 2010 Feb 14.

DOI:10.1016/j.bmcl.2010.02.050

PMID:20206516

Abstract

Utilizing a pharmacophore hypothesis, previously described gamma-secretase inhibiting HTS hits were evolved into novel tricyclic sulfonamide-pyrazoles, with high in vitro potency, good brain penetration, low metabolic stability, and high clearance.

摘要

利用药效基团假说，对之前描述的γ-分泌酶抑制高通量筛选命中化合物进行了衍生化，得到了新型三环磺酰胺-吡唑类化合物，具有高体外活性、良好的脑穿透性、低代谢稳定性和高清除率。

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磺酰胺-吡唑γ-分泌酶抑制剂的发现。

Discovery of sulfonamide-pyrazole gamma-secretase inhibitors.

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磺酰胺-吡唑γ-分泌酶抑制剂的发现。

Discovery of sulfonamide-pyrazole gamma-secretase inhibitors.

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