Literature DB >> 20630754

Synthesis and structure-activity relationship of N-(3-azabicyclo[3.1.0]hex-6-ylmethyl)-5-(2-pyridinyl)-1,3-thiazol-2-amines derivatives as NPY Y5 antagonists.

Matteo Biagetti1, Colin Philip Leslie, Angelica Mazzali, Catia Seri, Domenica Antonia Pizzi, Jonathan Bentley, Thorsten Genski, Romano Di Fabio, Laura Zonzini, Laura Caberlotto.   

Abstract

A novel class of small molecule NPY Y5 antagonists based around an azabicyclo[3.1.0]hexane scaffold was identified through modification of a screening hit. Structure-activity relationships and efforts undertaken to achieve a favourable pharmacokinetic profile in rat are described. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20630754     DOI: 10.1016/j.bmcl.2010.06.140

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


  2 in total

1.  NPY receptors as potential targets for anti-obesity drug development.

Authors:  Ernie Yulyaningsih; Lei Zhang; Herbert Herzog; Amanda Sainsbury
Journal:  Br J Pharmacol       Date:  2011-07       Impact factor: 8.739

2.  Synthesis of novel thiazole, pyranothiazole, thiazolo[4,5-b]pyridines and thiazolo[5',4':5,6]pyrano[2,3-d]pyrimidine derivatives and incorporating isoindoline-1,3-dione group.

Authors:  Mona A Hosny; Yasser H Zaki; Wafaa A Mokbel; Abdou O Abdelhamid
Journal:  BMC Chem       Date:  2019-03-26
  2 in total

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