ADP receptor inhibitors

ADP receptor inhibitors might be used in patients with coronary artery disease, in neurology, and in angiology. This chapter will mainly consider indications of ticlopidine and clopidogrel since these are the only two drugs currently available in the market. 

ADP receptor inhibitors play a major role in the management of ACS in interventional cardiology before and after stent... 

When 2-aminobenzothiazoles 204 (R = H, OMe, OEt, F, Cl, NO2, SO2NH2) are treated with 2 molar equiv of chlorosulfonylacetyl chloride and base, the fused 4//-l-thia-2,4-diazine 1,1-dioxides 205 result, which are of interest as potential platelet ADP receptor inhibitors (Equation 44) <1999W09939525>. 

Scarborough, R. M. Venkatraman, M. S. Zhang, X. Pandey, A. Preparation of substituted 2H-1,3-benzoxazin-4(3H)-ones as ADP receptor inhibitors for treating thrombosis and secondary ischemic events. U.S. Pat. Appl. Publ. US 2006069093, 2006 Chem. Abstr. 2006,144, 312098. 

The pharmacological treatment options for ACS include agents that either reduce oxygen demand (beta blockers) or increase oxygen supply (nitrates, potassium channel activators, calcium channel blockers) to the heart and antiplatelet (aspirin, ADP-receptor antagonists, GPIIb/llla receptor blockers) and antithrombin therapy (unfractionated heparin, low molecular weight heparin, direct thrombin inhibitors) (10). 

There are a number of additional targets that may lead to effective antithrombotic therapy in ACS. In terms of anticoagulants, the concepts of agents that have dual inhibitor sites such as the one we find in heparin but that lack in some of its undesirable qualities could be very useful. The same concept may apply to drugs that have both anticoagulant and antiplatelet properties, It is quite probable that inhibitors of tissue factor as well as of the platelet ADP receptor when combined with aspirin might be very effective. An ability to block the feedback action of the polyphosphates released from platelets upon activation is also an attractive aim (Fig. 3),... 

A. Classification and Prototypes Antiplatelet drugs include aspirin and other nonsteroidal anti-inflammatory dmgs (NSAIDs), dipyridamole and inhibitors of ADP receptors (ticlopidine and clopidogrel), and glycoprotein TIb/IIIa receptor inhibitors (abciximab, tirofiban, and epti-fibatide). These drugs increase bleeding time, a test used to monitor their effects. 

Antiplatelet agent that blocks ADP receptors irreversible inhibitor of fibrin binding to platelets. Used in transient ischemic attacks and to prevent strokes. Clopi-dogrel has a similar mechanism and use. Tox bleeding, diarrhea, leukopenia. 

Antagonists of the ADP P2Y, 2 receptor, ticlopidine and its safer successor clopidogrel, are also potent inhibitors of platelet aggregation and have demonstrated their efficacy alone and on top of ASA in numerous in clinical studies. The results of the CAPRIE study, a large study involving 19,185 patients with recent Ml, stroke, or established peripheral arterial disease (PAD) demonstrated an 8.7% overall risk reduction versus ASA in the combined endpoints of the first occurrence of Ml, stroke, or other vascular death (30). 

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