Literature DB >> 15978811

Discovery and SAR of biaryl piperidine MCH1 receptor antagonists through solid-phase encoded combinatorial synthesis.

Tao Guo1, Yuefei Shao, Gang Qian, Laura L Rokosz, Tara M Stauffer, Rachael C Hunter, Suresh D Babu, Huizhong Gu, Doug W Hobbs.   

Abstract

An encoded combinatorial library based on aryl and biaryl piperidine scaffolds was designed and synthesized. Screening of this library resulted in the discovery of high-nanomolar biaryl piperidine-based MCH1 receptor antagonists. Follow-up optimization using a parallel synthesis provided potent, single digit nanomolar antagonists.

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Year:  2005        PMID： 15978811     DOI： 10.1016/j.bmcl.2005.05.085

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


  1 in total

1.  Optimization of biaryl piperidine and 4-amino-2-biarylurea MCH1 receptor antagonists using QSAR modeling, classification techniques and virtual screening.

Authors:  Georgia Melagraki; Antreas Afantitis; Haralambos Sarimveis; Panayiotis A Koutentis; John Markopoulos; Olga Igglessi-Markopoulou
Journal:  J Comput Aided Mol Des       Date:  2007-03-22       Impact factor: 4.179
  1 in total

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