Ono, Shin’ichiro published the artcilePreparation and pharmacological evaluation of novel glycoprotein (Gp) IIb/IIIa antagonists. 2. Condensed heterocyclic derivatives, Application of Ethyl 6-cyano-1H-indole-2-carboxylate, the main research area is benzofuran preparation structure integrin antagonist antithrombotic; platelet aggregation inhibitor integrin receptor antagonist; prodrug amidinobenzofuran integrin antagonist antithrombotic.
A novel series of platelet receptor glycoprotein (Gp) IIb/IIIa antagonists with condensed heterocycles as their basic core was synthesized. In an in vitro assay, trans-4-(5-amidinobenzofuran-2-carboxamido)cyclohexyloxyacetic acid (I) and trans-3-[4-(5-amidinobenzofuran-2-carboxamido)cyclohexyl]propionic acid (II) produced marked inhibitions with IC50 values of 0.018 and 0.006 μM, resp., in a human platelet adenosine-5′-diphospate (ADP)-induced aggregation assay; they also exhibited a wide spectrum of inhibition toward major aggregation agonists (ADP, collagen, thrombin, PMA (tumor promoter) and arachidonic acid). These compounds were >2-3 orders of magnitude more effective in inhibiting platelet aggregation than human umbilical vein endothelial cell (HUVEC) binding. The oral administration of 10 mg/kg of either I and II to guinea pig, resulted in a 60% inhibition of ex vivo platelet aggregation after 5 h. Oral administration of Et trans-4-(5-amidinobenzofuran-2-carboxamido)cyclohexyloxyacetate (III) (10 mg/kg) resulted in 80% inhibition of platelet aggregation in dogs for 6 h after oral administration with a return to baseline by 24 h. Et trans-3-[4-(5-amidinobenzofuran-2-carboxamido)cyclohexyl]propionate (AR0598) produced 80% inhibition for 5 h after oral administration. Prodrug III showed a good profile in dogs with a long duration of action. III (AR0510) was selected as suitable clin. candidate for development as an orally active antithrombotic agent.
Chemical & Pharmaceutical Bulletin published new progress about Anticoagulants. 104291-81-8 belongs to class indole-building-block, name is Ethyl 6-cyano-1H-indole-2-carboxylate, and the molecular formula is C12H10N2O2, Application of Ethyl 6-cyano-1H-indole-2-carboxylate.
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles