Literature DB >> 15615511

Discovery of tetralin carboxamide growth hormone secretagogue receptor antagonists via scaffold manipulation.

Hongyu Zhao1, Zhili Xin, Gang Liu, Verlyn G Schaefer, H Douglas Falls, Wiweka Kaszubska, Christine A Collins, Hing L Sham.   

Abstract

A case study of rational design of an efficient, specific, and proprietary molecular scaffold based on the structure-activity relationship (SAR) information on a screening hit is described. Potent, selective, and orally bioavailable tetralin carboxamide growth hormone secretagogue receptor (GHS-R) antagonists were discovered. Union of rational design and high throughput synthesis provided a quick access to high quality chemical leads.

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Year:  2004        PMID: 15615511     DOI: 10.1021/jm0491750

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  4 in total

1.  ScafBank: a public comprehensive Scaffold database to support molecular hopping.

Authors:  Bi-Bo Yan; Meng-Zhu Xue; Bing Xiong; Ke Liu; Ding-Yu Hu; Jing-Kang Shen
Journal:  Acta Pharmacol Sin       Date:  2009-01-19       Impact factor: 6.150

Review 2.  Constitutive activation of G protein-coupled receptors and diseases: insights into mechanisms of activation and therapeutics.

Authors:  Ya-Xiong Tao
Journal:  Pharmacol Ther       Date:  2008-08-09       Impact factor: 12.310

3.  Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists.

Authors:  Suvi T M Orr; Ramsay Beveridge; Samit K Bhattacharya; Kimberly O Cameron; Steven Coffey; Dilinie Fernando; David Hepworth; Margaret V Jackson; Vishal Khot; Rachel Kosa; Kimberly Lapham; Paula M Loria; Kim F McClure; Jigna Patel; Colin Rose; James Saenz; Ingrid A Stock; Gregory Storer; Maria von Volkenburg; Derek Vrieze; Guoqiang Wang; Jun Xiao; Yingxin Zhang
Journal:  ACS Med Chem Lett       Date:  2014-12-14       Impact factor: 4.345

Review 4.  Approved and Off-Label Uses of Obesity Medications, and Potential New Pharmacologic Treatment Options.

Authors:  Mª Luisa Isidro; Fernando Cordido
Journal:  Pharmaceuticals (Basel)       Date:  2010-01-12
  4 in total

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