Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators

Cheruvallath, Zacharia S.; Gwaltney, II, Stephen L.; Sabat, Mark; Tang, Mingnam; Wang, Haixia; Jennings, Andy; Hosfield, David; Lee, Bumsup; Wu, Yiqin; Halkowycz, Petro; Grimshaw, Charles E.

doi:10.1016/j.bmcl.2017.04.041

Title: Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators

Journal Article · Thu Jun 01 00:00:00 EDT 2017 · Bioorganic and Medicinal Chemistry Letters

DOI:https://doi.org/10.1016/j.bmcl.2017.04.041· OSTI ID:1416584

Cheruvallath, Zacharia S.; Gwaltney, II, Stephen L.; Sabat, Mark; Tang, Mingnam; Wang, Haixia; Jennings, Andy; Hosfield, David; Lee, Bumsup; Wu, Yiqin; Halkowycz, Petro; Grimshaw, Charles E.

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Sponsoring Organization:: USDOE

OSTI ID:: 1416584

Journal Information:: Bioorganic and Medicinal Chemistry Letters, Journal Name: Bioorganic and Medicinal Chemistry Letters Vol. 27 Journal Issue: 12; ISSN 0960-894X

Publisher:: ElsevierCopyright Statement

Country of Publication:: United Kingdom

Language:: English

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Cited by: 16 works

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References (14)

Type 2 diabetes market Gershell, Leland Nature Reviews Drug Discovery, Vol. 4, Issue 5 https://doi.org/10.1038/nrd1723	journal	May 2005
Drugs, QT Interval Prolongation and ICH E14: The Need to Get it Right Shah, Rashmi R. Drug Safety, Vol. 28, Issue 2 https://doi.org/10.2165/00002018-200528020-00003	journal	January 2005
Initial Management of Glycemia in Type 2 Diabetes Mellitus Nathan, David M. New England Journal of Medicine, Vol. 347, Issue 17 https://doi.org/10.1056/NEJMcp021106	journal	October 2002
Insulin sensitisation in the treatment of Type 2 diabetes Tadayyon, M.; Smith, Sa Expert Opinion on Investigational Drugs, Vol. 12, Issue 3 https://doi.org/10.1517/13543784.12.3.307	journal	March 2003
Design, synthesis and SAR of novel glucokinase activators Cheruvallath, Zacharia S.; Gwaltney, Stephen L.; Sabat, Mark Bioorganic & Medicinal Chemistry Letters, Vol. 23, Issue 7 https://doi.org/10.1016/j.bmcl.2013.01.093	journal	April 2013
Glucokinase Activators for Diabetes Therapy: May 2010 status report Matschinsky, F. M.; Zelent, B.; Doliba, N. Diabetes Care, Vol. 34, Issue Supplement_2 https://doi.org/10.2337/dc11-s236	journal	April 2011
Glycemic Control With Diet, Sulfonylurea, Metformin, or Insulin in Patients With Type 2 Diabetes MellitusProgressive Requirement for Multiple Therapies (UKPDS 49) Turner, Robert C. JAMA, Vol. 281, Issue 21 https://doi.org/10.1001/jama.281.21.2005	journal	June 1999
Insights into the Structure and Regulation of Glucokinase from a Novel Mutation (V62M), Which Causes Maturity-onset Diabetes of the Young Gloyn, Anna L.; Odili, Stella; Zelent, Dorothy Journal of Biological Chemistry, Vol. 280, Issue 14 https://doi.org/10.1074/jbc.M413146200	journal	April 2005
A Comparison of Agents Used to Manage Type 2 Diabetes Mellitus: Need for Reappraisal of Traditional Approaches Bell, David S. H. Treatments in Endocrinology, Vol. 3, Issue 2 https://doi.org/10.2165/00024677-200403020-00001	journal	January 2004
Small molecule glucokinase activators as novel anti-diabetic agents Leighton, B.; Atkinson, A.; Coghlan, M. P. Biochemical Society Transactions, Vol. 33, Issue 2 https://doi.org/10.1042/BST0330371	journal	April 2005
Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle Pfefferkorn, Jeffrey A.; Lou, Jihong; Minich, Martha L. Bioorganic & Medicinal Chemistry Letters, Vol. 19, Issue 12 https://doi.org/10.1016/j.bmcl.2009.04.107	journal	June 2009
Glucokinase and glucose homeostasis: proven concepts and new ideas Zelent, D.; Najafi, H.; Odili, S. Biochemical Society Transactions, Vol. 33, Issue 1 https://doi.org/10.1042/BST0330306	journal	February 2005
Regulation of Pancreatic -Cell Glucokinase: From Basics to Therapeutics Matschinsky, F. M. Diabetes, Vol. 51, Issue Supplement 3 https://doi.org/10.2337/diabetes.51.2007.S394	journal	December 2002
Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis Cumming, John G.; Tucker, Howard; Oldfield, John Bioorganic & Medicinal Chemistry Letters, Vol. 22, Issue 4 https://doi.org/10.1016/j.bmcl.2011.12.117	journal	February 2012

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