Literature DB >> 22300657

Hit to lead SAR study on benzoxazole derivatives for an NPY Y5 antagonist.

Naoki Omori1, Naoki Kouyama, Akira Yukimasa, Kana Watanabe, Yasunori Yokota, Hideki Tanioka, Hirohide Nambu, Hideo Yukioka, Norihito Sato, Yukari Tanaka, Kazutaka Sekiguchi, Takayuki Okuno.   

Abstract

We report a hit to lead study on a novel benzoxazole NPY Y5 antagonist. Starting from HTS hit 1, structure-activity relationships were developed. Compound 12 showed reduction of food intake and a tendency to suppress body weight gain over the 21-day experimental period.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 22300657     DOI: 10.1016/j.bmcl.2012.01.027

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


  5 in total

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Authors:  Gilbert W Kim; Jieru E Lin; Erik S Blomain; Scott A Waldman
Journal:  Expert Opin Drug Discov       Date:  2013-04-29       Impact factor: 6.098

Review 2.  Appetite Regulation: Hormones, Peptides, and Neurotransmitters and Their Role in Obesity.

Authors:  Gary D Miller
Journal:  Am J Lifestyle Med       Date:  2017-06-23

Review 3.  Antiobesity pharmacotherapy: new drugs and emerging targets.

Authors:  G W Kim; J E Lin; E S Blomain; S A Waldman
Journal:  Clin Pharmacol Ther       Date:  2013-10-08       Impact factor: 6.875

Review 4.  Can neuropeptides treat obesity? A review of neuropeptides and their potential role in the treatment of obesity.

Authors:  C K Boughton; K G Murphy
Journal:  Br J Pharmacol       Date:  2013-12       Impact factor: 8.739

Review 5.  Importance of Fluorine in Benzazole Compounds.

Authors:  Thuraya Al-Harthy; Wajdi Zoghaib; Raid Abdel-Jalil
Journal:  Molecules       Date:  2020-10-14       Impact factor: 4.411

  5 in total

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