Total synthesis of a thromboxane receptor antagonist, terutroban

2015 ◽  
Vol 13 (10) ◽  
pp. 2951-2957 ◽  
Author(s):  
Wasim Ahmed ◽  
Prathama S. Mainkar ◽  
Srihari Pabbaraja ◽  
Srivari Chandrasekhar
Keyword(s):  
Total Synthesis ◽  
Receptor Antagonist ◽  
Cost Effective ◽  
Diels Alder ◽  
Thromboxane Receptor ◽  
Thromboxane Receptor Antagonist

Synthesis of terutroban (2) is achieved following a non-Diels–Alder approach using cost-effective chemicals.

Synergistic Antiplatelet Effect of Ridogrel, a Combined Thromboxane Receptor Antagonist and Thromboxane Synthase Inhibitor, and UDCG-212, a cAMP-Phosphodiesterase Inhibitor

1993 ◽  
Vol 70 (05) ◽  
pp. 822-825 ◽  
Author(s):  
B Hoet ◽  
J Arnout ◽  
H Deckmyn ◽  
J Vermylen
Keyword(s):  
Arachidonic Acid ◽  
Platelet Aggregation ◽  
Receptor Antagonist ◽  
Phosphodiesterase Inhibitor ◽  
Camp Phosphodiesterase ◽  
Thromboxane Receptor ◽  
Thromboxane Synthase Inhibitor ◽  
Thromboxane Receptor Antagonist ◽  
Synthase Inhibitor ◽  
Camp Levels

SummaryRidogrel, a combined thromboxane receptor antagonist and thromboxane synthase inhibitor (1), inhibits platelet aggregation. Following stimulation with arachidonic acid, cAMP-levels are increased in human platelets preincubated with ridogrel, this is due to the known reorientation of the metabolism of the formed endoperoxides towards adenylate cyclase stimulating prostaglandins.Pretreatment of resting platelets with UDCG-212, a cAMP-phosphodiesterase inhibitor (2), also inhibits platelet aggregation induced by arachidonic acid, concomitant with an increase in cAMP levels, due to an inhibition of its breakdown. Under basal conditions, cAMP also is increased.By combining the two drugs, a more than additive action was observed on platelet aggregation and on both resting and stimulated platelet cAMP content. The appropriate combination may result in a more effective antiplatelet strategy.

Sign in / Sign up

Export Citation Format

Share Document