Literature DB >> 25437504

Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists I.

Juan Antonio Alonso1, Miriam Andrés1, Mónica Bravo1, Maria Antonia Buil1, Marta Calbet1, Jordi Castro1, Paul R Eastwood2, Peter Eichhorn1, Cristina Esteve1, Elena Gómez1, Jacob González1, Marta Mir1, Silvia Petit1, Richard S Roberts1, Bernat Vidal1, Laura Vidal1, Pere Vilaseca1, Miriam Zanuy1.   

Abstract

A knowledge-based design strategy led to the discovery of several new series of potent and orally bioavailable CRTh2 antagonists where a bicyclic heteroaromatic ring serves as the central core. Structure-kinetic relationships (SKR) opened up the possibility of long receptor residence times.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  CRTh2 antagonist; Receptor residence time; Structure–activity relationship (SAR); Structure–kinetic relationship (SKR)

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Year:  2014        PMID： 25437504     DOI： 10.1016/j.bmcl.2014.09.005

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


  1 in total

1.  Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma.

Authors:  David A Sandham; Lucy Barker; Lyndon Brown; Zarin Brown; David Budd; Steven J Charlton; Devnandan Chatterjee; Brian Cox; Gerald Dubois; Nicholas Duggan; Edward Hall; Julia Hatto; Janet Maas; Jodie Manini; Rachael Profit; Darren Riddy; Catherine Ritchie; Bindi Sohal; Duncan Shaw; Rowan Stringer; David A Sykes; Matthew Thomas; Katharine L Turner; Simon J Watson; Ryan West; Elisabeth Willard; Gareth Williams; Jennifer Willis
Journal:  ACS Med Chem Lett       Date:  2017-04-25       Impact factor: 4.345
  1 in total

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