Novel tricyclic benzothiazolo[2,3-c]thiadiazine antagonists of the platelet ADP receptor (P2Y(12))

R M Scarborough; A M Laibelman; L A Clizbe; L J Fretto; P B Conley; E E Reynolds; D M Sedlock; H Jantzen

doi:10.1016/s0960-894x(01)00313-4

Novel tricyclic benzothiazolo[2,3-c]thiadiazine antagonists of the platelet ADP receptor (P2Y(12))

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1805-8. doi: 10.1016/s0960-894x(01)00313-4.

Authors

R M Scarborough¹, A M Laibelman, L A Clizbe, L J Fretto, P B Conley, E E Reynolds, D M Sedlock, H Jantzen

Affiliation

¹ COR Therapeutics, Inc., Departments of Medicinal Chemistry and Biology, 94080, South San Francisco, CA, USA. rscarborough@corr.com

PMID: 11459636
DOI: 10.1016/s0960-894x(01)00313-4

Abstract

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.

MeSH terms

Adenosine Diphosphate / metabolism
Binding Sites / drug effects
Binding Sites / physiology
Heterocyclic Compounds / chemical synthesis*
Heterocyclic Compounds / pharmacology*
Humans
Inhibitory Concentration 50
Membrane Proteins*
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*

Substances

CT 50547
Heterocyclic Compounds
Membrane Proteins
P2RY12 protein, human
Platelet Aggregation Inhibitors
Purinergic P2 Receptor Antagonists
Receptors, Purinergic P2Y12
Thiadiazines
Thiazoles
Adenosine Diphosphate