Literature DB >> 12852954

3-(2-Benzyloxyphenyl)isoxazoles and isoxazolines: synthesis and evaluation as CFTR activators.

Robert E Sammelson1, T Ma, Luis J V Galietta, A S Verkman, Mark J Kurth.   

Abstract

A novel class of activators for chloride conductance in the cystic fibrosis transmembrane conductance regulator (CFTR) protein has been identified. These 3-(2-benzyloxyphenyl)isoxazoles and 3-(2-benzyloxyphenyl)isoxazolines were synthesized employing the 1,3-dipolar cycloaddition of nitrile oxides with various alkene and alkyne dipolarophiles. Utilizing a fluorescence cell-based assay of halide transport, the best compounds increased CFTR-dependent chloride transport with half-maximal stimulation at 20-50 microM.

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Year:  2003        PMID： 12852954     DOI： 10.1016/s0960-894x(03)00482-7

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


  6 in total

Review 1.  CFTR pharmacology.

Authors:  Olga Zegarra-Moran; Luis J V Galietta
Journal:  Cell Mol Life Sci       Date:  2016-10-04       Impact factor: 9.261

2.  Regulatory domain phosphorylation to distinguish the mechanistic basis underlying acute CFTR modulators.

Authors:  Louise C Pyle; Annette Ehrhardt; Lisa High Mitchell; Lijuan Fan; Aixia Ren; Anjaparavanda P Naren; Yao Li; J P Clancy; Graeme B Bolger; Eric J Sorscher; Steven M Rowe
Journal:  Am J Physiol Lung Cell Mol Physiol       Date:  2011-07-01       Impact factor: 5.464

3.  Expedient synthesis of a 72-membered isoxazolino-β-ketoamide library by a 2·3-component reaction.

Authors:  John M Knapp; Jie S Zhu; Alex B Wood; Mark J Kurth
Journal:  ACS Comb Sci       Date:  2012-01-03       Impact factor: 3.784

4.  CFTR potentiators partially restore channel function to A561E-CFTR, a cystic fibrosis mutant with a similar mechanism of dysfunction as F508del-CFTR.

Authors:  Yiting Wang; Jia Liu; Avgi Loizidou; Luc A Bugeja; Ross Warner; Bethan R Hawley; Zhiwei Cai; Ashley M Toye; David N Sheppard; Hongyu Li
Journal:  Br J Pharmacol       Date:  2014-09-05       Impact factor: 8.739

Review 5.  Cystic fibrosis transmembrane conductance regulator modulators for personalized drug treatment of cystic fibrosis: progress to date.

Authors:  Frédéric Becq
Journal:  Drugs       Date:  2010-02-12       Impact factor: 9.546

6.  Differential thermostability and response to cystic fibrosis transmembrane conductance regulator potentiators of human and mouse F508del-CFTR.

Authors:  Samuel J Bose; Marcel J C Bijvelds; Yiting Wang; Jia Liu; Zhiwei Cai; Alice G M Bot; Hugo R de Jonge; David N Sheppard
Journal:  Am J Physiol Lung Cell Mol Physiol       Date:  2019-04-10       Impact factor: 5.464
  6 in total

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