title: Carbazole-containing sulfonamides and sulfamides: Discovery of cryptochrome modulators as antidiabetic agents.
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.
authors.affiliation: Reset Therapeutics, 260 Littlefield Avenue, Suite 200, South San Francisco, CA 94080, USA. Electronic address: paul@resettherapeutics.com.
authors.forename: Paul S
authors.initials: PS
authors.lastname: Humphries
authors.affiliation: Reset Therapeutics, 260 Littlefield Avenue, Suite 200, South San Francisco, CA 94080, USA.
authors.forename: Ross
authors.initials: R
authors.lastname: Bersot
authors.affiliation: Synterys Inc., 29540 Kohoutek Way, Union City, CA 94587, USA.
authors.forename: John
authors.initials: J
authors.lastname: Kincaid
authors.affiliation: Reset Therapeutics, 260 Littlefield Avenue, Suite 200, South San Francisco, CA 94080, USA.
authors.forename: Eric
authors.initials: E
authors.lastname: Mabery
authors.affiliation: Reset Therapeutics, 260 Littlefield Avenue, Suite 200, South San Francisco, CA 94080, USA.
authors.forename: Kerryn
authors.initials: K
authors.lastname: McCluskie
authors.affiliation: Reset Therapeutics, 260 Littlefield Avenue, Suite 200, South San Francisco, CA 94080, USA.
authors.forename: Timothy
authors.initials: T
authors.lastname: Park
authors.affiliation: Reset Therapeutics, 260 Littlefield Avenue, Suite 200, South San Francisco, CA 94080, USA.
authors.forename: Travis
authors.initials: T
authors.lastname: Renner
authors.affiliation: Reset Therapeutics, 260 Littlefield Avenue, Suite 200, South San Francisco, CA 94080, USA.
authors.forename: Erin
authors.initials: E
authors.lastname: Riegler
authors.affiliation: Reset Therapeutics, 260 Littlefield Avenue, Suite 200, South San Francisco, CA 94080, USA.
authors.forename: Tod
authors.initials: T
authors.lastname: Steinfeld
authors.affiliation: Synterys Inc., 29540 Kohoutek Way, Union City, CA 94587, USA.
authors.forename: Eric D
authors.initials: ED
authors.lastname: Turtle
authors.affiliation: Synterys Inc., 29540 Kohoutek Way, Union City, CA 94587, USA.
authors.forename: Zhi-Liang
authors.initials: ZL
authors.lastname: Wei
authors.affiliation: Reset Therapeutics, 260 Littlefield Avenue, Suite 200, South San Francisco, CA 94080, USA.
authors.forename: Erik
authors.initials: E
authors.lastname: Willis
mesh_terms: D000818:Animals; D001786:Blood Glucose / Q000032:analysis; D002227:Carbazoles / Q000737:chemistry*; D045744:Cell Line, Tumor; D056931:Cryptochromes / Q000737:chemistry* / Q000235:genetics / Q000378:metabolism; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy / Q000473:pathology; D059305:Diet, High-Fat; D005786:Gene Expression Regulation / Q000187:drug effects; D017930:Genes, Reporter; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D051379:Mice; D008810:Mice, Inbred C57BL; D008820:Mice, Obese; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D001786:Blood Glucose; D002227:Carbazoles; D056931:Cryptochromes; D007004:Hypoglycemic Agents; D013449:Sulfonamides; C041514:carbazole
keywords: Carbazole; Circadian; Cryptochrome; Diabetes; SAR