Carbazole-containing sulfonamides and sulfamides: Discovery of cryptochrome modulators as antidiabetic agents

Bioorg Med Chem Lett. 2016 Feb 1;26(3):757-760. doi: 10.1016/j.bmcl.2015.12.102.

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 ³, Zhi-Liang Wei ³, Erik Willis ²

Affiliations

1 Reset Therapeutics, 260 Littlefield Avenue, Suite 200, South San Francisco, CA 94080, USA. Electronic address: [email protected].
2 Reset Therapeutics, 260 Littlefield Avenue, Suite 200, South San Francisco, CA 94080, USA.
3 Synterys Inc., 29540 Kohoutek Way, Union City, CA 94587, USA.

PMID: 26778255 DOI: 10.1016/j.bmcl.2015.12.102

Abstract

A series of novel carbazole-containing sulfonamides and sulfamides were synthesized. A structure-activity relationship study of these compounds led to the identification of potent Cryptochrome modulators. Based on the results of efficacy studies in diet-induced obese (DIO) mice, and the desired pharmacokinetic parameters, compound 41 was selected for further profiling.

Keywords

Carbazole; Circadian; Cryptochrome; Diabetes; SAR.

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