Literature DB >> 19896843

Tetrahydroquinoline derivatives as CRTH2 antagonists.

Jiwen Liu1, Yingcai Wang, Ying Sun, Derek Marshall, Shichang Miao, George Tonn, Penny Anders, Joel Tocker, H Lucy Tang, Julio Medina.   

Abstract

A series of tetrahydroquinoline-derived inhibitors of the CRTH2 receptor was discovered by a high throughput screen. Optimization of these compounds for potency and pharmacokinetic properties led to the discovery of potent and orally bioavailable CRTH2 antagonists.

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Year:  2009        PMID: 19896843     DOI: 10.1016/j.bmcl.2009.10.094

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


  5 in total

1.  Synthesis of an azide-tagged library of 2,3-dihydro-4-quinolones.

Authors:  Hajoong Lee; Masato Suzuki; Jiayue Cui; Sergey A Kozmin
Journal:  J Org Chem       Date:  2010-03-05       Impact factor: 4.354

2.  Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.

Authors:  Jiwen Liu; An-Rong Li; Yingcai Wang; Mike G Johnson; Yongli Su; Wang Shen; Xuemei Wang; Sarah Lively; Matthew Brown; SuJen Lai; Felix Gonzalez Lopez De Turiso; Qingge Xu; Bettina Van Lengerich; Mike Schmitt; Zice Fu; Ying Sun; Shanna Lawlis; Lisa Seitz; Jay Danao; Jill Wait; Qiuping Ye; Hua Lucy Tang; Mark Grillo; Tassie L Collins; Timothy J Sullivan; Julio C Medina
Journal:  ACS Med Chem Lett       Date:  2011-03-02       Impact factor: 4.345

3.  Benzodiazepinone Derivatives as CRTH2 Antagonists.

Authors:  Jiwen Jim Liu; Alan C Cheng; H Lucy Tang; Julio C Medina
Journal:  ACS Med Chem Lett       Date:  2011-04-17       Impact factor: 4.345

4.  Discovery of a Novel Series of CRTH2 (DP2) Receptor Antagonists Devoid of Carboxylic Acids.

Authors:  Stefano Crosignani; Catherine Jorand-Lebrun; Gordon Campbell; Adeline Prêtre; Tania Grippi-Vallotton; Anna Quattropani; Gwenaelle Bouscary-Desforges; Agnes Bombrun; Marc Missotten; Yves Humbert; Christèle Frémaux; Mikaël Pâquet; Kamel El Harkani; Charles G Bradshaw; Christophe Cleva; Nada Abla; Hamina Daff; Olivier Schott; Pierre-André Pittet; Jean-François Arrighi; Marilène Gaudet; Zoë Johnson
Journal:  ACS Med Chem Lett       Date:  2011-10-10       Impact factor: 4.345

5.  Discovery of MK-8318, a Potent and Selective CRTh2 Receptor Antagonist for the Treatment of Asthma.

Authors:  Xianhai Huang; Jason Brubaker; Wei Zhou; Purakkattle J Biju; Li Xiao; Ning Shao; Ying Huang; Li Dong; Zhidan Liu; Rema Bitar; Alexei Buevich; Joon Jung; Scott L Peterson; John W Butcher; Joshua Close; Michelle Martinez; Rachel N MacCoss; Hongjun Zhang; Scott Crawford; Kevin D McCormick; Robert Aslanian; Ravi Nargund; Craig Correll; Francois Gervais; Hongchen Qiu; Xiaoxin Yang; Charles Garlisi; Diane Rindgen; Kevin M Maloney; Phieng Siliphaivanh; Anandan Palani
Journal:  ACS Med Chem Lett       Date:  2018-06-23       Impact factor: 4.345

  5 in total

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