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

被引:23
作者
Scarborough, RM [1 ]
Laibelman, AM
Clizbe, LA
Fretto, LJ
Conley, PB
Reynolds, EE
Sedlock, DM
Jantzen, HM
机构
[1] COR Therapeut Inc, Dept Med Chem, S San Francisco, CA 94080 USA
[2] COR Therapeut Inc, Dept Biol, S San Francisco, CA 94080 USA
关键词
D O I
10.1016/S0960-894X(01)00313-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Novel non-nucleoside tricyclic platelet ADP receptor (P2Y(12)) antagonists hat e 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. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1805 / 1808
页数:4
相关论文
共 11 条
[1]   Aspirin [J].
Awtry, EH ;
Loscalzo, J .
CIRCULATION, 2000, 101 (10) :1206-1218
[2]   Molecular basis for ADP-induced platelet activation I. Evidence for three distinct ADP receptors on human platelets [J].
Daniel, JL ;
Dangelmaier, C ;
Jin, JG ;
Ashby, B ;
Smith, JB ;
Kunapuli, SP .
JOURNAL OF BIOLOGICAL CHEMISTRY, 1998, 273 (04) :2024-2029
[3]   Identification of the platelet ADP receptor targeted by antithrombotic drugs [J].
Hollopeter, G ;
Jantzen, HM ;
Vincent, D ;
Li, G ;
England, L ;
Ramakrishnan, V ;
Yang, RB ;
Nurden, P ;
Nurden, A ;
Julius, D ;
Conley, PB .
NATURE, 2001, 409 (6817) :202-207
[4]   A NOVEL SERIES OF P-2T PURINOCEPTOR ANTAGONISTS - DEFINITION OF THE ROLE OF ADP IN ARTERIAL THROMBOSIS [J].
HUMPHRIES, RG ;
ROBERTSON, MJ ;
LEFF, P .
TRENDS IN PHARMACOLOGICAL SCIENCES, 1995, 16 (06) :179-181
[5]   PHARMACOLOGICAL PROFILE OF THE NOVEL P-2T-PURINOCEPTOR ANTAGONIST, FPL-67085 IN-VITRO AND IN THE ANESTHETIZED RAT IN-VIVO [J].
HUMPHRIES, RG ;
TOMLINSON, W ;
CLEGG, JA ;
INGALL, AH ;
KINDON, ND ;
LEFF, P .
BRITISH JOURNAL OF PHARMACOLOGY, 1995, 115 (06) :1110-1116
[6]   Antagonists of the platelet P2T receptor:: A novel approach to antithrombotic therapy [J].
Ingall, AH ;
Dixon, J ;
Bailey, A ;
Coombs, ME ;
Cox, D ;
McInally, JI ;
Hunt, SF ;
Kindon, ND ;
Teobald, BJ ;
Willis, PA ;
Humphries, RG ;
Leff, P ;
Clegg, JA ;
Smith, JA ;
Tomlinson, W .
JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (02) :213-220
[7]  
Jantzen HM, 1999, THROMB HAEMOSTASIS, V81, P111
[8]   Ticlopidine and clopidogrel [J].
Quinn, MJ ;
Fitzgerald, DJ .
CIRCULATION, 1999, 100 (15) :1667-1672
[9]   Identification and biological activity of the active metabolite of clopidogrel [J].
Savi, P ;
Pereillo, JM ;
Uzabiaga, MF ;
Combalbert, J ;
Picard, C ;
Maffrand, JP ;
Pascal, M ;
Herbert, JM .
THROMBOSIS AND HAEMOSTASIS, 2000, 84 (05) :891-896
[10]  
SAVI P, 1994, J PHARMACOL EXP THER, V269, P772