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Rational Design and Synthesis of 4-substituted 2-pyridin-2-ylamides With Inhibitory Effects on SH2 Domain-Containing Inositol 5'-phosphatase 2 (SHIP2)

Rational Design and Synthesis of 4-substituted 2-pyridin-2-ylamides With Inhibitory Effects on SH2 Domain-Containing Inositol 5'-phosphatase 2 (SHIP2)

Yoshinori Ichihara, Ryohei Fujimura, Hiroshi Tsuneki, Tsutomu Wada, Kentaro Okamoto, Hiroaki Gouda, Shuichi Hirono, Kenji Sugimoto, Yuji Matsuya, Toshiyasu Sasaoka, Naoki Toyooka

Eur J Med Chem. 2013 Apr;62:649-60.

PMID: 23434638

Abstract:

Novel 4-substituted 2-pyridin-2-ylamides were developed using in-silico ligand-based drug design (LBDD) in an attempt to identify inhibitors of SH2-containing 5'-inositol phosphatase 2 (SHIP2), which is implicated in insulin-resistant type 2 diabetes. Among the compounds synthesized, N-[4-(4-chlorobenzyloxy)pyridin-2-yl]-2-(2,6-difluorophenyl)- acetamide (CPDA, 4a) was identified as a potent SHIP2 inhibitor. CPDA was found to enhance in vitro insulin signaling through the Akt pathway more efficiently than the previously reported SHIP2 inhibitor AS1949490, and ameliorated abnormal glucose metabolism in diabetic (db/db) mice.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1203680765	AS1949490		1203680-76-5	Price

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