Literature DB >> 18602261

Synthesis and structure-activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: a novel series of 5-HT2C receptor antagonists.

Chul Min Park1, So Young Kim, Woo Kyu Park, No Sang Park, Churl Min Seong.   

Abstract

A novel series of 1H-indole-3-carboxylic acid pyridine-3-ylamides were synthesized and identified to show high affinity and selectivity for 5-HT(2C) receptor. Among them, 1H-indole-3-carboxylic acid[6-(2-chloro-pyridin-3-yloxy)-pyridin-3-yl]-amide (15k) exhibits the highest affinity (IC(50)=0.5 nM) with an excellent selectivity (>2000 times) over other serotonin (5-HT(1A), 5-HT(2A), and 5-HT(6)) and dopamine (D(2)-D(4)) receptors.

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Year:  2008        PMID： 18602261     DOI： 10.1016/j.bmcl.2008.06.064

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


  3 in total

1.  Insights into binding modes of 5-HT2c receptor antagonists with ligand-based and receptor-based methods.

Authors:  Chunhua Lu; Fangfang Jin; Cui Li; Weihua Li; Guixia Liu; Yun Tang
Journal:  J Mol Model       Date:  2011-01-04       Impact factor: 1.810

2.  A new biarylphosphine ligand for the Pd-catalyzed synthesis of diaryl ethers under mild conditions.

Authors:  Luca Salvi; Nicole R Davis; Siraj Z Ali; Stephen L Buchwald
Journal:  Org Lett       Date:  2011-12-19       Impact factor: 6.005

3.  Synthesis and Evaluation of Pyridyloxypyridyl Indole Carboxamides as Potential PET Imaging Agents for 5-HT2C Receptors.

Authors:  Fanxing Zeng; Jonathon A Nye; Ronald J Voll; Leonard Howell; Mark M Goodman
Journal:  ACS Med Chem Lett       Date:  2018-02-05       Impact factor: 4.345
  3 in total

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