Literature DB >> 11606139

Synthesis of 1-benzyl-3-(5'-hydroxymethyl-2'-furyl)indazole analogues as novel antiplatelet agents.

F Y Lee1, J C Lien, L J Huang, T M Huang, S C Tsai, C M Teng, C C Wu, F C Cheng, S C Kuo.   

Abstract

1-Benzyl-3-(5'-hydroxymethyl-2'-furyl)indazole (28, YC-1) was selected as the lead compound for systemic structural modification. After screening for antiplatelet activity, SARs of YC-1 analogues were established. Among these potent active derivatives, compounds 29, 30, 31, 44, and 45 functioned as potent activators of sGC and inhibitors of PDE5 with potency comparable to that of YC-1. In addition, compound 58 was found to be a selective and potent inhibitor of protease-activated receptor type 4 (PAR4)-dependent platelet activation.

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Year:  2001        PMID： 11606139     DOI： 10.1021/jm010001h

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


  18 in total

Review 1.  NO-independent stimulators and activators of soluble guanylate cyclase: discovery and therapeutic potential.

Authors:  Oleg V Evgenov; Pál Pacher; Peter M Schmidt; György Haskó; Harald H H W Schmidt; Johannes-Peter Stasch
Journal:  Nat Rev Drug Discov       Date:  2006-09       Impact factor: 84.694

2.  Development of a Series of (1-Benzyl-3-(6-methoxypyrimidin-3-yl)-5-(trifluoromethoxy)-1H-indol-2-yl)methanols as Selective Protease Activated Receptor 4 (PAR4) Antagonists with in Vivo Utility and Activity Against γ-Thrombin.

Authors:  Kayla J Temple; Matthew T Duvernay; Summer E Young; Wandong Wen; Wenjun Wu; Jae G Maeng; Anna L Blobaum; Shaun R Stauffer; Heidi E Hamm; Craig W Lindsley
Journal:  J Med Chem       Date:  2016-08-08       Impact factor: 7.446

3.  Identification of the minimum PAR4 inhibitor pharmacophore and optimization of a series of 2-methoxy-6-arylimidazo[2,1-b][1,3,4]thiadiazoles.

Authors:  Kayla J Temple; Matthew T Duvernay; Jae G Maeng; Anna L Blobaum; Shaun R Stauffer; Heidi E Hamm; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2016-10-11       Impact factor: 2.823

4.  Discovery and Optimization of a Novel Series of Competitive and Central Nervous System-Penetrant Protease-Activated Receptor 4 (PAR4) Inhibitors.

Authors:  Jeanette L Bertron; Matthew T Duvernay; Sidnee G Mitchell; Shannon T Smith; Jae G Maeng; Anna L Blobaum; Dexter C Davis; Jens Meiler; Heidi E Hamm; Craig W Lindsley
Journal:  ACS Chem Neurosci       Date:  2021-12-02       Impact factor: 4.418

5.  Late-stage ortho-C-H alkenylation of 2-arylindazoles in aqueous medium by Manganese(i)-catalysis.

Authors:  Krishna Kanta Das; Asim Kumar Ghosh; Alakananda Hajra
Journal:  RSC Adv       Date:  2022-07-04       Impact factor: 4.036

6.  Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354.

Authors:  Wandong Wen; Summer E Young; Matthew T Duvernay; Michael L Schulte; Kellie D Nance; Bruce J Melancon; Julie Engers; Charles W Locuson; Michael R Wood; J Scott Daniels; Wenjun Wu; Craig W Lindsley; Heidi E Hamm; Shaun R Stauffer
Journal:  Bioorg Med Chem Lett       Date:  2014-08-15       Impact factor: 2.823

7.  A Robust Protocol for Pd(II)-catalyzed C-3 Arylation of (1H) Indazoles and Pyrazoles: Total Synthesis of Nigellidine Hydrobromide.

Authors:  Mengchun Ye; Andrew J F Edmunds; James A Morris; David Sale; Yejia Zhang; Jin-Quan Yu
Journal:  Chem Sci       Date:  2013-06-01       Impact factor: 9.825

Review 8.  Protease-activated receptor 4: from structure to function and back again.

Authors:  Shauna L French; Justin R Hamilton
Journal:  Br J Pharmacol       Date:  2016-03-10       Impact factor: 8.739

9.  Synthesis and structure-activity relationship studies of novel 3,9-substituted α-carboline derivatives with high cytotoxic activity against colorectal cancer cells.

Authors:  Yi-Chien Lin; Yi-Fong Chen; Li-Shin Tseng; Yueh-Hsuan Lee; Susan L Morris-Natschke; Sheng-Chu Kuo; Ning-Sun Yang; Kuo-Hsiung Lee; Li-Jiau Huang
Journal:  Eur J Med Chem       Date:  2016-01-07       Impact factor: 6.514

10.  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
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