Literature DB >> 19818611

Rapid access towards follow-up NOP receptor agonists using a knowledge based approach.

Ronald Palin1, John K Clark, Louise Evans, Helen Feilden, Dan Fletcher, Niall M Hamilton, Andrea K Houghton, Philip S Jones, Duncan McArthur, Brian Montgomery, Paul D Ratcliffe, Alasdair R C Smith, Aaron Sutherland, Mark A Weston, Grant Wishart.   

Abstract

A knowledge based approach has been adopted to identify novel NOP receptor agonists with simplified hydrophobes. Substitution of the benzimidazol-2-one piperidine motif with a range of hydrophobic groups and pharmacophore guided bio-isosteric replacement of the benzimidazol-2-one moiety was explored. Compound 51 was found to be a high affinity, potent NOP receptor agonist with reduced affinity for the hERG channel.

Entities:  

Mesh:

Substances:

Year:  2009        PMID: 19818611     DOI: 10.1016/j.bmcl.2009.09.028

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


  2 in total

1.  In silico study of the structurally similar ORL1 receptor agonist and antagonist pairs reveal possible mechanism of receptor activation.

Authors:  Milan Senćanski; Ljiljana Dosen-Mićović
Journal:  Protein J       Date:  2014-06       Impact factor: 2.371

2.  Synthesis and Selective Functionalization of Thiadiazine 1,1-Dioxides with Efficacy in a Model of Huntington's Disease.

Authors:  Leila Terrab; Christopher J Rosenker; Lisa Johnstone; Linh K Ngo; Li Zhang; Nathaniel F Ware; Bettina Miller; Andrea Z Topacio; Sara Sannino; Jeffrey L Brodsky; Peter Wipf
Journal:  ACS Med Chem Lett       Date:  2020-02-20       Impact factor: 4.345

  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.