Literature DB >> 26778255

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

Paul S Humphries1, Ross Bersot2, John Kincaid3, Eric Mabery2, Kerryn McCluskie2, Timothy Park2, Travis Renner2, Erin Riegler2, Tod Steinfeld2, Eric D Turtle3, Zhi-Liang Wei3, Erik Willis2.   

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.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Carbazole; Circadian; Cryptochrome; Diabetes; SAR

Mesh:

Substances:

Year:  2015        PMID: 26778255     DOI: 10.1016/j.bmcl.2015.12.102

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  17 in total

1.  Cryptochromes-Mediated Inhibition of the CRL4Cop1-Complex Assembly Defines an Evolutionary Conserved Signaling Mechanism.

Authors:  Luca Rizzini; Daniel C Levine; Mark Perelis; Joseph Bass; Clara B Peek; Michele Pagano
Journal:  Curr Biol       Date:  2019-05-30       Impact factor: 10.834

2.  DNA binding and cleavage, BRCA1 gene interaction, antiglycation and anticancer studies of transition metal complexes of sulfonamides.

Authors:  Arusa Akhtar; Muhammad Danish; Awais Asif; Muhammad Nadeem Arshad; Abdullah M Asiri
Journal:  Mol Divers       Date:  2022-02-19       Impact factor: 2.943

3.  A wrinkle in time: circadian biology in pulmonary vascular health and disease.

Authors:  Andrew J Bryant; Elnaz Ebrahimi; Amy Nguyen; Christopher A Wolff; Michelle L Gumz; Andrew C Liu; Karyn A Esser
Journal:  Am J Physiol Lung Cell Mol Physiol       Date:  2021-12-01       Impact factor: 5.464

Review 4.  Circadian Etiology of Type 2 Diabetes Mellitus.

Authors:  Naureen Javeed; Aleksey V Matveyenko
Journal:  Physiology (Bethesda)       Date:  2018-03-01

Review 5.  Development and Therapeutic Potential of Small-Molecule Modulators of Circadian Systems.

Authors:  Zheng Chen; Seung-Hee Yoo; Joseph S Takahashi
Journal:  Annu Rev Pharmacol Toxicol       Date:  2017-10-02       Impact factor: 13.820

Review 6.  Circadian clocks and insulin resistance.

Authors:  Dirk Jan Stenvers; Frank A J L Scheer; Patrick Schrauwen; Susanne E la Fleur; Andries Kalsbeek
Journal:  Nat Rev Endocrinol       Date:  2019-02       Impact factor: 43.330

7.  Blockade of alcohol excessive and "relapse" drinking in male mice by pharmacological cryptochrome (CRY) activation.

Authors:  Yan Zhou; Mary Jeanne Kreek
Journal:  Psychopharmacology (Berl)       Date:  2021-01-08       Impact factor: 4.530

Review 8.  The circadian clock and liver function in health and disease.

Authors:  Atish Mukherji; Shannon M Bailey; Bart Staels; Thomas F Baumert
Journal:  J Hepatol       Date:  2019-03-28       Impact factor: 30.083

9.  Structure property relationships of N-acylsulfonamides and related bioisosteres.

Authors:  Karol R Francisco; Carmine Varricchio; Thomas J Paniak; Marisa C Kozlowski; Andrea Brancale; Carlo Ballatore
Journal:  Eur J Med Chem       Date:  2021-03-28       Impact factor: 7.088

Review 10.  Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review.

Authors:  Chuang Zhao; K P Rakesh; L Ravidar; Wan-Yin Fang; Hua-Li Qin
Journal:  Eur J Med Chem       Date:  2018-11-22       Impact factor: 6.514

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