1,2,3,4-四氢异喹啉基氨基磺酸作为磷酸酶PTP1B抑制剂

1,2,3,4-Tetrahydroisoquinolinyl sulfamic acids as phosphatase PTP1B inhibitors.

作者信息

Klopfenstein Sean R, Evdokimov Artem G, Colson Anny-Odile, Fairweather Neil T, Neuman Jeffrey J, Maier Matthew B, Gray Jeffrey L, Gerwe Gina S, Stake George E, Howard Brian W, Farmer Julie A, Pokross Matthew E, Downs Thomas R, Kasibhatla Bhavani, Peters Kevin G

机构信息

Procter & Gamble Pharmaceuticals, Health Care Research Center, 8700 Mason-Montgomery Road, Mason, OH 45040, USA.

出版信息

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1574-8. doi: 10.1016/j.bmcl.2005.12.051. Epub 2006 Jan 4.

DOI:10.1016/j.bmcl.2005.12.051

PMID:16386905

Abstract

High-throughput screening of the P&GP corporate repository against several protein tyrosine phosphatases identified the sulfamic acid moiety as potential phosphotyrosine mimetic. Incorporation of the sulfamic acid onto a 1,2,3,4-tetrahydroisoquinoline scaffold provided a promising starting point for PTP1B inhibitor design.

摘要

针对多种蛋白酪氨酸磷酸酶对P&GP公司文库进行高通量筛选，确定氨基磺酸部分为潜在的磷酸酪氨酸模拟物。将氨基磺酸引入1,2,3,4-四氢异喹啉骨架为设计PTP1B抑制剂提供了一个有前景的起点。