Literature DB >> 17314044

2,5-Disubstituted pyridines: the discovery of a novel series of 5-HT2A ligands.

Kevin J Wilson1, Monique B van Niel, Laura Cooper, Dawn Bloomfield, Desmond O'Connor, L Rebecca Fish, Angus M MacLeod.   

Abstract

This report describes the effect of replacing the central basic amine present in many known 5-HT(2A) ligands with an aromatic residue. We targeted the isomeric phenethylpyridines 2 and 3 and these compounds proved to be excellent leads, possessing good 5-HT(2A) receptor binding affinity and selectivity over the 5-HT(2C) subtype. Optimization of one isomer led to the identification of 25, a compound with sub-nanomolar 5-HT(2A) affinity and selectivity over 5-HT(2C) of greater than 4600-fold.

Entities:  

Mesh：

Substances：

Year:  2007        PMID： 17314044     DOI： 10.1016/j.bmcl.2007.01.098

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


  2 in total

1.  An atom-economical addition of methyl azaarenes with aromatic aldehydes via benzylic C(sp3)-H bond functionalization under solvent- and catalyst-free conditions.

Authors:  Divya Rohini Yennamaneni; Vasu Amrutham; Krishna Sai Gajula; Rammurthy Banothu; Murali Boosa; Narender Nama
Journal:  Beilstein J Org Chem       Date:  2020-12-23       Impact factor: 2.883

2.  Hetero-Diels-Alder reaction of 1,3-bis(trimethylsilyloxy)-1,3-butadienes with arylsulfonylcyanides. Synthesis and antimicrobial activity of 4-hydroxy-2-(arylsulfonyl)pyridines.

Authors:  Ibrar Hussain; Mirza Arfan Yawer; Michael Lalk; Ulrike Lindequist; Alexander Villinger; Christine Fischer; Peter Langer
Journal:  Bioorg Med Chem       Date:  2008-10-17       Impact factor: 3.641
  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.