- 1,2,3,4-Tetrahydroisoquinolinyl sulfamic acids as phosphatase PTP1B inhibitors.
1,2,3,4-Tetrahydroisoquinolinyl sulfamic acids as phosphatase PTP1B inhibitors.
Bioorganic & medicinal chemistry letters (2006-01-03)
Sean R Klopfenstein, Artem G Evdokimov, Anny-Odile Colson, Neil T Fairweather, Jeffrey J Neuman, Matthew B Maier, Jeffrey L Gray, Gina S Gerwe, George E Stake, Brian W Howard, Julie A Farmer, Matthew E Pokross, Thomas R Downs, Bhavani Kasibhatla, Kevin G Peters
PMID16386905
摘要
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.
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