Literature DB >> 16380251

Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists.

Martin C Clasby1, Samuel Chackalamannil, Michael Czarniecki, Dario Doller, Keith Eagen, William J Greenlee, Yan Lin, Hsingan Tsai, Yan Xia, Ho-Sam Ahn, Jacqueline Agans-Fantuzzi, George Boykow, Madhu Chintala, Carolyn Foster, Matthew Bryant, Janice Lau.   

Abstract

The design, synthesis, and SAR studies of a structurally novel series of highly potent thrombin receptor (PAR-1) antagonists are described. Compound 30 is a highly potent thrombin receptor antagonist (IC(50)=6.3 nM), a related compound 36 showing efficacy in a monkey ex vivo study.

Entities:  

Mesh：

Substances：

Year:  2005        PMID： 16380251     DOI： 10.1016/j.bmcl.2005.12.042

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


  3 in total

1.  Copper-Catalyzed Synthesis of Hindered Ethers from α-Bromo Carbonyl Compounds.

Authors:  Zhe Zhou; Nicole Erin Behnke; László Kürti
Journal:  Org Lett       Date:  2018-08-16       Impact factor: 6.005

2.  Facile synthesis of 7-alkyl-1,2,3,4-tetrahydro-1,8-naphthyridines as arginine mimetics using a Horner-Wadsworth-Emmons-based approach.

Authors:  Rhys A Lippa; John A Murphy; Tim N Barrett
Journal:  Beilstein J Org Chem       Date:  2020-07-08       Impact factor: 2.883

3.  Synthesis of indole derived protease-activated receptor 4 antagonists and characterization in human platelets.

Authors:  Summer E Young; Matthew T Duvernay; Michael L Schulte; Craig W Lindsley; Heidi E Hamm
Journal:  PLoS One       Date:  2013-06-11       Impact factor: 3.240
  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.