2. Academic Validation
  3. Carbazole-containing amides and ureas: Discovery of cryptochrome modulators as antihyperglycemic agents

Carbazole-containing amides and ureas: Discovery of cryptochrome modulators as antihyperglycemic agents

  • Bioorg Med Chem Lett. 2018 Feb 1;28(3):293-297. doi: 10.1016/j.bmcl.2017.12.051.
Paul S Humphries 1,  Ross Bersot 2,  John Kincaid 3,  Eric Mabery 2,  Kerryn McCluskie 2,  Timothy Park 2,  Travis Renner 2,  Erin Riegler 2,  Tod Steinfeld 2,  Eric D Turtle 2,  Zhi-Liang Wei 3,  Erik Willis 2
Affiliations

Affiliations

  • 1 Reset Therapeutics, 260 Littlefield Avenue, Suite 200, South San Francisco, CA 94080, USA. Electronic address: paul@resettherapeutics.com.
  • 2 Reset Therapeutics, 260 Littlefield Avenue, Suite 200, South San Francisco, CA 94080, USA.
  • 3 Synterys, 29540 Kohoutek Way, Union City, CA 94587, USA.
PMID: 29292223 DOI: 10.1016/j.bmcl.2017.12.051
Abstract

A series of novel carbazole-containing amides and ureas were synthesized. A structure-activity relationship study of these compounds led to the identification of potent Cryptochrome modulators. Based on the desired pharmacokinetic/pharmacodynamic parameters and the results of efficacy studies in db/db mice, compound 50 was selected for further profiling.

Keywords

Carbazole; Circadian; Cryptochrome; Diabetes; SAR.

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