Literature DB >> 14998320

Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor.

Katherine L Widdowson1, John D Elliott, Daniel F Veber, Hong Nie, Melvin C Rutledge, Brent W McCleland, Jia-Ning Xiang, Anthony J Jurewicz, Robert P Hertzberg, James J Foley, Don E Griswold, Lenox Martin, Judithann M Lee, John R White, Henry M Sarau.   

Abstract

N,N'-Diarylureas were prepared, and the structure-activity relationship relative to the CXCR2 receptor was examined. This led to the identification of a potent and highly selective CXCR2 antagonist, which in addition was shown to be functionally active both in vitro against human neutrophils and in vivo in rabbit models of ear edema and neutropenia.

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Year:  2004        PMID: 14998320     DOI: 10.1021/jm034248l

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


  14 in total

1.  Aryltriflates as a Neglected Moiety in Medicinal Chemistry: A Case Study from a Lead Optimization of CXCL8 Inhibitors.

Authors:  Alessio Moriconi; Chiara Bigogno; Gianluca Bianchini; Antonio Caligiuri; Anna Resconi; Massimo G Dondio; Gaetano D'Anniballe; Marcello Allegretti
Journal:  ACS Med Chem Lett       Date:  2011-08-07       Impact factor: 4.345

2.  In vitro inhibition of translation initiation by N,N'-diarylureas--potential anti-cancer agents.

Authors:  Séverine Denoyelle; Ting Chen; Limo Chen; Yibo Wang; Edvin Klosi; José A Halperin; Bertal H Aktas; Michael Chorev
Journal:  Bioorg Med Chem Lett       Date:  2011-11-16       Impact factor: 2.823

Review 3.  Current concepts on oxidative/carbonyl stress, inflammation and epigenetics in pathogenesis of chronic obstructive pulmonary disease.

Authors:  Hongwei Yao; Irfan Rahman
Journal:  Toxicol Appl Pharmacol       Date:  2011-02-04       Impact factor: 4.219

4.  Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders.

Authors:  Heng Xu; Hongfu Lu; Zhongmiao Xu; Linbo Luan; Chengyong Li; Yan Xu; Kelly Dong; Jinqiang Zhang; Xiong Li; Yvonne Li; Gentao Liu; Sophie Gong; Yong-Gang Zhao; Ailian Liu; Yueting Zhang; Wei Zhang; Xin Cai; Jia-Ning Xiang; John D Elliott; Xichen Lin
Journal:  ACS Med Chem Lett       Date:  2016-02-08       Impact factor: 4.345

5.  Critical role of endothelial CXCR2 in LPS-induced neutrophil migration into the lung.

Authors:  Jörg Reutershan; Margaret A Morris; Tracy L Burcin; David F Smith; Daniel Chang; Mary S Saprito; Klaus Ley
Journal:  J Clin Invest       Date:  2006-02-16       Impact factor: 14.808

6.  SB265610 is an allosteric, inverse agonist at the human CXCR2 receptor.

Authors:  M E Bradley; M E Bond; J Manini; Z Brown; S J Charlton
Journal:  Br J Pharmacol       Date:  2009-04-24       Impact factor: 8.739

Review 7.  Biology and therapeutic potential of cannabinoid CB2 receptor inverse agonists.

Authors:  C A Lunn; E-P Reich; J S Fine; B Lavey; J A Kozlowski; R W Hipkin; D J Lundell; L Bober
Journal:  Br J Pharmacol       Date:  2007-10-01       Impact factor: 8.739

Review 8.  International Union of Basic and Clinical Pharmacology. [corrected]. LXXXIX. Update on the extended family of chemokine receptors and introducing a new nomenclature for atypical chemokine receptors.

Authors:  Francoise Bachelerie; Adit Ben-Baruch; Amanda M Burkhardt; Christophe Combadiere; Joshua M Farber; Gerard J Graham; Richard Horuk; Alexander Hovard Sparre-Ulrich; Massimo Locati; Andrew D Luster; Alberto Mantovani; Kouji Matsushima; Philip M Murphy; Robert Nibbs; Hisayuki Nomiyama; Christine A Power; Amanda E I Proudfoot; Mette M Rosenkilde; Antal Rot; Silvano Sozzani; Marcus Thelen; Osamu Yoshie; Albert Zlotnik
Journal:  Pharmacol Rev       Date:  2013-11-11       Impact factor: 25.468

Review 9.  Role of angiogenesis and vascular remodeling in chronic obstructive pulmonary disease.

Authors:  Nikolaos M Siafakas; Katerina M Antoniou; Eleni G Tzortzaki
Journal:  Int J Chron Obstruct Pulmon Dis       Date:  2007

10.  Inhibition of LPS-induced airway neutrophilic inflammation in healthy volunteers with an oral CXCR2 antagonist.

Authors:  Brian R Leaker; Peter J Barnes; Brian O'Connor
Journal:  Respir Res       Date:  2013-12-16
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