PTP1B inhibition and antihyperglycemic activity in the ob/ob mouse model of novel 11-arylbenzo[b]naphtho[2,3-d]furans and 11-arylbenzo[b]naphtho[2,3- d]thiophenes

Jay Wrobel, Janet Sredy, Christopher Moxham, Arlene Dietrich, Zenan Li, Diane R. Sawicki, Laura Seestaller, Li Wu, Alan Katz, Donald Sullivan, Cesario Tio, Zhong Yin Zhang

Research output: Contribution to journalArticle

121 Scopus citations

Abstract

We have reported on a series of novel, potent, and selective PTPase inhibitors that function as oral antidiabetic agents. Compounds 6 and 7 are particularly notable in this regard. They were both low nanomolar inhibitors and lowered glucose in the diabetic ob/ob mouse at doses at or below 10 mg/kg/day, po. Compound 7 generally showed selectivities against other PTPases of greater than 25-fold. These compounds and other analogues are currently being further evaluated.

Original languageEnglish (US)
Pages (from-to)3199-3202
Number of pages4
JournalJournal of Medicinal Chemistry
Volume42
Issue number17
DOIs
StatePublished - Aug 26 1999
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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