Synthesis and biological evaluation of 9,11-azo-13-oxa-15-hydroxyprostanoic acid, a potent inhibitor of platelet aggregation

1979 ◽  
Vol 22 (11) ◽  
pp. 1402-1408 ◽  
Author(s):  
Sheung-Tsam Kam ◽  
Philip S. Portoghese ◽  
Jonathan M. Gerrard ◽  
Earl W. Dunham
Keyword(s):  
Platelet Aggregation ◽  
Potent Inhibitor ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

Design, synthesis and biological evaluation of novel ligustrazinylated derivatives as potent cardiovascular agents

MedChemComm ◽  
2013 ◽  
Vol 4 (5) ◽  
pp. 827-832 ◽  
Author(s):  
Hongfei Chen ◽  
Guoning Li ◽  
Peng Zhan ◽  
Xiuli Guo ◽  
Qian Ding ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Protective Effect ◽  
Biological Evaluation ◽  
Cardiovascular Agents ◽  
Design Synthesis ◽  
Platelet Aggregation Inhibition ◽  
Aggregation Inhibition ◽  
Synthesis And Biological Evaluation

A series of novel ligustrazinylated derivatives was designed, synthesized and evaluated for their platelet aggregation inhibition and protective effect on injured ECV-304 cells.

Synthesis and biological evaluation of N-(2-fluorophenyl)-2β-deoxyfuconojirimycin acetamide as a potent inhibitor for α-l-fucosidases

2013 ◽  
Vol 21 (21) ◽  
pp. 6565-6573 ◽  
Author(s):  
Atsushi Kato ◽  
Toru Okaki ◽  
Syohei Ifuku ◽  
Kasumi Sato ◽  
Yuki Hirokami ◽  
...  
Keyword(s):  
Potent Inhibitor ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

scholarly journals Synthesis and Biological Evaluation of Novel Jatrorrhizine Derivatives with Amino Groups Linked at the 3-Position as Inhibitors of Acetylcholinesterase

2017 ◽  
Vol 2017 ◽  
pp. 1-6 ◽  
Author(s):  
Xiaofei Jiang ◽  
Nengling Zhang ◽  
Nanqian Xiong ◽  
Yi Liu ◽  
Jianfeng Cao ◽  
...  
Keyword(s):  
Potent Inhibitor ◽  
Biological Evaluation ◽  
Lead Compound ◽  
Amino Groups ◽  
Coptis Chinensis ◽  
Inhibitor Activity ◽  
Active Constituents ◽  
Potential Inhibitors ◽  
Synthesis And Biological Evaluation

Jatrorrhizine was considered as one of the active constituents of Coptis chinensis Franch. Herein, jatrorrhizine derivatives with substituted amino groups linked at the 3-position were designed, synthesized, and biologically evaluated as inhibitors of acetylcholinesterase. Jatrorrhizine derivatives inhibited the activity of acetylcholinesterase (AChE) to a greater extent than the lead compound jatrorrhizine. All these jatrorrhizine derivatives were proved to be potent inhibitors of acetylcholinesterase (AChE) with submicromolar IC50 values, but less sensitive to butyrylcholinesterase (BuChE), which suggests that these jatrorrhizine derivatives are selective for AChE/BuChE. Compound 3g gave the most potent inhibitor activity for AChE (IC50 = 0.301 μM), which is greater than the lead compound jatrorrhizine. All these results demonstrated that these jatrorrhizine derivatives are potential inhibitors for AChE.

scholarly journals Synthesis and biological evaluation of n-butylphthalide derivatives as anti-platelet aggregation agents

2016 ◽  
Vol 30 (23) ◽  
pp. 2716-2719 ◽  
Author(s):  
Meihui Chen ◽  
Qi Liu ◽  
Min Tan ◽  
Shijun Wen ◽  
Rongbiao Pi ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

scholarly journals Cyclopamine analogs bearing exocyclic methylenes are highly potent and acid-stable inhibitors of hedgehog signaling

2013 ◽  
Vol 9 ◽  
pp. 2328-2335 ◽  
Author(s):  
Johann Moschner ◽  
Anna Chentsova ◽  
Nicole Eilert ◽  
Irene Rovardi ◽  
Philipp Heretsch ◽  
...  
Keyword(s):  
Nitrogen Atom ◽  
Hedgehog Signaling ◽  
Potent Inhibitor ◽  
Biological Evaluation ◽  
Luciferase Expression ◽  
Acid Stability ◽  
Methyl Group ◽  
F Ring ◽  
Synthesis And Biological Evaluation ◽  
Acid Stable

The chemical synthesis and biological evaluation of new cyclopamine analogs bearing exocyclic methylenes in different positions is described. Bis-exo-cyclopamine 6 was identified as a potent inhibitor of the Gli1-dependent luciferase expression in Shh-LIGHTII cells. An extension of this study to F-ring-modified structures shows the necessity of a rigidly positioned nitrogen atom for bioactivity as well as the presence of the C21 methyl group for acid stability and bioactivity.

Synthesis and Biological Evaluation of Bridged Analogues of the Platelet Aggregation Inhibitor Trifenagrel

2009 ◽  
Vol 6 (7) ◽  
pp. 478-486
Author(s):  
Magdalena Slusarczyk ◽  
Wim De Borggraeve ◽  
Georges Hoornaert ◽  
Koen Robeyns ◽  
Luc Meervelt ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Biological Evaluation ◽  
Platelet Aggregation Inhibitor ◽  
Aggregation Inhibitor ◽  
Synthesis And Biological Evaluation
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