Literature DB >> 17064898

Structure-activity relationships of novel non-competitive mGluR1 antagonists: a potential treatment for chronic pain.

Dafydd R Owen1, Peter G Dodd, Simon Gayton, Ben S Greener, Gareth W Harbottle, Simon J Mantell, Graham N Maw, Simon A Osborne, Huw Rees, Tracy J Ringer, Margarita Rodriguez-Lens, Graham F Smith.   

Abstract

A series of novel mGluR1 antagonists have been prepared. Incorporation of fragments derived from weak lead matter into a library led to enhanced potency in a new chemical series. A chemistry driven second library iteration, covering a greatly enhanced area of chemical space, maintained good potency and introduced metabolic stability.

Entities:  

Mesh:

Substances:

Year:  2006        PMID: 17064898     DOI: 10.1016/j.bmcl.2006.10.015

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


  2 in total

Review 1.  Recent advances in the medicinal chemistry of the metabotropic glutamate receptor 1 (mGlu₁).

Authors:  Dafydd R Owen
Journal:  ACS Chem Neurosci       Date:  2011-03-10       Impact factor: 4.418

2.  A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors.

Authors:  Hyekyung P Cho; Darren W Engers; Daryl F Venable; Colleen M Niswender; Craig W Lindsley; P Jeffrey Conn; Kyle A Emmitte; Alice L Rodriguez
Journal:  ACS Chem Neurosci       Date:  2014-05-15       Impact factor: 4.418

  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.