Literature DB >> 8667356

Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists.

H Riechers1, H P Albrecht, W Amberg, E Baumann, H Bernard, H J Böhm, D Klinge, A Kling, S Müller, M Raschack, L Unger, N Walker, W Wernet.   

Abstract

A novel class of endothelin-A receptor ligands was discovered by high-throughput screening. Lead structure optimization led to highly potent antagonists which can be synthesized in a short sequence. The compounds are endothelin-A-selective, are orally available, and show a long duration of action.

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Year:  1996        PMID: 8667356     DOI: 10.1021/jm960274q

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  10 in total

Review 1.  Impact of high-throughput screening in biomedical research.

Authors:  Ricardo Macarron; Martyn N Banks; Dejan Bojanic; David J Burns; Dragan A Cirovic; Tina Garyantes; Darren V S Green; Robert P Hertzberg; William P Janzen; Jeff W Paslay; Ulrich Schopfer; G Sitta Sittampalam
Journal:  Nat Rev Drug Discov       Date:  2011-03       Impact factor: 84.694

2.  The inadequacy of the reductionist approach in discovering new therapeutic agents against complex diseases.

Authors:  Manuel X Duval
Journal:  Exp Biol Med (Maywood)       Date:  2018-08-08

3.  Effect of endothelin and endothelin receptor blockade on capillary permeability in experimental pancreatitis.

Authors:  G Eibl; H G Hotz; J Faulhaber; M Kirchengast; H J Buhr; T Foitzik
Journal:  Gut       Date:  2000-03       Impact factor: 23.059

4.  Selective endothelin A receptor antagonism with sitaxentan reduces neointimal lesion size in a mouse model of intraluminal injury.

Authors:  Karolina M Duthie; Patrick W F Hadoke; Nicholas S Kirkby; Eileen Miller; Jessica R Ivy; John F McShane; Win Gel Lim; David J Webb
Journal:  Br J Pharmacol       Date:  2015-04-23       Impact factor: 8.739

5.  Endothelin ETA receptor blockade restores NO-mediated endothelial function and inhibits atherosclerosis in apolipoprotein E-deficient mice.

Authors:  M Barton; C C Haudenschild; L V d'Uscio; S Shaw; K Münter; T F Lüscher
Journal:  Proc Natl Acad Sci U S A       Date:  1998-11-24       Impact factor: 11.205

6.  Endothelin receptor blockade improves fluid sequestration, pancreatic capillary blood flow, and survival in severe experimental pancreatitis.

Authors:  T Foitzik; J Faulhaber; H G Hotz; M Kirchengast; H J Buhr
Journal:  Ann Surg       Date:  1998-11       Impact factor: 12.969

7.  The role of endothelin-1 as a mediator of the pressure response after air embolism in blood perfused lungs.

Authors:  J Schmeck; T Koch; B Patt; A Heller; H Neuhof; K van Ackern
Journal:  Intensive Care Med       Date:  1998-06       Impact factor: 17.440

Review 8.  The endothelin system as a therapeutic target in cardiovascular disease: great expectations or bleak house?

Authors:  N S Kirkby; P W F Hadoke; A J Bagnall; D J Webb
Journal:  Br J Pharmacol       Date:  2007-10-29       Impact factor: 8.739

9.  (3,4-Dimeth-oxy-phen-yl)(4-fluoro-phen-yl)methanone.

Authors:  Quanjian Lv; Jianling Wang
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-06-05

10.  Ambrisentan for the treatment of pulmonary arterial hypertension.

Authors:  Brian Casserly; James R Klinger
Journal:  Drug Des Devel Ther       Date:  2009-02-06       Impact factor: 4.162

  10 in total

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