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

Academic Article
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Overview

authors

  • Cheruvallath, Z. S.
  • Gwaltney, S. L.
  • Sabat, M.
  • Tang, M.
  • Wang, H.
  • Jennings, A.
  • Hosfield, David J
  • Lee, B.
  • Wu, Y.
  • Halkowycz, P.
  • Grimshaw, C. E.

publication date

  • June 2017

journal

  • Bioorganic & Medicinal Chemistry Letters  Journal

subject areas

  • Administration, Oral
  • Allosteric Regulation
  • Animals
  • Diabetes Mellitus, Experimental
  • Diabetes Mellitus, Type 2
  • Dose-Response Relationship, Drug
  • Drug Discovery
  • Enzyme Activators
  • Ether-A-Go-Go Potassium Channels
  • Glucokinase
  • Glucose Tolerance Test
  • Humans
  • Indazoles
  • Mice
  • Mice, Inbred C57BL
  • Mice, Obese
  • Models, Molecular
  • Molecular Structure
  • Potassium Channel Blockers
  • Structure-Activity Relationship
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Research

keywords

  • 1,4-Disubstituted indazole
  • Glucokinase activator
  • OGTT
  • Structure-based drug design
  • Type 2 diabetes
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Identity

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2017.04.041

PubMed ID

  • 28512030
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Additional Document Info

start page

  • 2678

end page

  • 2682

volume

  • 27

issue

  • 12

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