CLOPIDOGREL AND TICAGRELOR: A NOVEL FUSED RING OF FIVE MEMBER WITH SIX MEMBER HETEROCYCLIC CLASS AS ORALLY ACTIVE ANTICOAGULANT

Abstract

Clopidogrel and ticagrelor both drugs have fused ring heterocyclic moiety of five+six member entity having chiral centres. Clopidogrel have thieno-piperidine nucleus having one chiral carbon and ticlagrelor has triazolo-pyrimidine ring having four chiral centres. Both of the drugs act as anticoagulant by inhibiting the receptor P2Y₁₂. This protein is found mainly but not exclusively on the surface of blood platelets, and is an important regulator in blood clotting. P2Y₁₂ belongs to the Gi class of a group of G protein coupled (GPCR) purinergic receptors and is a chemoreceptor for adenosine diphosphate (ADP). The P2Y family has several receptor subtypes with different pharmacological selectivity, which overlaps in some cases, for various adenosine and uridine nucleotides. This receptor is involved in platelet aggregation, and is a potential target for the treatment of thromboembolisms and other clotting disorders. Two transcript variants encoding the same isoform have been identified for this gene.

KEYWORDS: P2Y₁₂, ADP, GPCR, Clopidogrel, Ticagrelor, Hemorrhage, Neutropenia, Thrombotic thrombocytopenic purpura, Coagulation