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Bioorg Med Chem Lett. 2018 Feb 1;28(3):293-297. doi: 10.1016/j.bmcl.2017.12.051. Epub 2017 Dec 24.

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

Author information

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.

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

PMID:
29292223
DOI:
10.1016/j.bmcl.2017.12.051

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