Novel tricyclic benzothiazolo[2,3-c]thiadiazine antagonists of the platelet ADP receptor (P2Y12)

• Published in: Bioorganic & medicinal chemistry letters Vol. 11; no. 14; pp. 1805 - 1808
• Main Authors: SCARBOROUGH, Robert M, LAIBELMAN, Alan M, CLIZBE, Lane A, FRETTO, Larry J, CONLEY, Pamela B, REYNOLDS, Elwood E, SEDLOCK, David M, JANTZEN, Hans-Michael
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier 23-07-2001
• Subjects: Adenosine Diphosphate - metabolism; Binding Sites - drug effects; Binding Sites - physiology; Biological and medical sciences; Blood. Blood coagulation. Reticuloendothelial system; Heterocyclic Compounds - chemical synthesis; Heterocyclic Compounds - pharmacology; Humans; Inhibitory Concentration 50; Medical sciences; Membrane Proteins; Pharmacology. Drug treatments; Platelet Aggregation - drug effects; Platelet Aggregation Inhibitors - chemistry; Platelet Aggregation Inhibitors - pharmacology; Purinergic P2 Receptor Antagonists; Radioligand Assay; Receptors, Purinergic P2Y12; Thiadiazines - chemical synthesis; Thiadiazines - pharmacology; Thiazoles - chemical synthesis; Thiazoles - pharmacology; Screening; Structure activity relation; Non nucleoside compound; Chemical compound library; Combinatorial chemistry; P2 Purinergic receptor; Antagonist; Chemical synthesis; In vitro; Antiplatelet agent
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/S0960-894X(01)00313-4

Novel non-nucleoside tricyclic platelet ADP receptor (P2Y(12)) antagonists have been discovered that bind reversibly and with high affinity to the platelet receptor. Condensation of various 2-aminobenzothiazoles with chlorosulfonylacetyl chloride affords these novel tricyclic heterocycles, which are novel and unpredicted products of this reaction.