scholarly journals Structure-activity relationships of novel 3-acylpyrrole derivatives: New inhibitors of platelet aggregation.

1980 ◽  
Vol 3 (11) ◽  
pp. 589-602
Author(s):  
AKIRA OHTSU ◽  
TOSHIO TANAKA ◽  
FUKUYOSHI KAMIMOTO ◽  
KENJI HOSHINA ◽  
SEIZI KUROZUMI ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Structure Activity Relationships ◽  
Structure Activity

Structure–activity relationships of chalcone analogs as potential inhibitors of ADP- and collagen-induced platelet aggregation

2011 ◽  
Vol 19 (24) ◽  
pp. 7711-7719 ◽  
Author(s):  
M. Vijaya Bhaskar Reddy ◽  
Wei-Jern Tsai ◽  
Keduo Qian ◽  
Kuo-Hsiung Lee ◽  
Tian-Shung Wu
Keyword(s):  
Platelet Aggregation ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Potential Inhibitors

Structure-activity relationships of αIIb313-320 derived peptide inhibitors of human platelet aggregation

2008 ◽  
Vol 14 (11) ◽  
pp. 1195-1202 ◽  
Author(s):  
Ruxandra Maria Stanica ◽  
Dimitra Benaki ◽  
Foteini I. Rodis ◽  
Emmanuel Mikros ◽  
Dimokritos Tsoukatos ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Human Platelet ◽  
Peptide Inhibitors ◽  
Structure Activity Relationships ◽  
Human Platelet Aggregation ◽  
Structure Activity

Qualititative Structure Activity Relationships In Serveral New Types Of Oral Anticoagulants

1981 ◽  
Author(s):  
k Rehse ◽  
R Bienfait ◽  
U Emisch ◽  
W Kapp ◽  
W Schinkel ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Oral Administration ◽  
Anticoagulant Activity ◽  
Oral Anticoagulants ◽  
Heterocyclic Ring ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Single Oral Administration

Various 1, 2-benzoxathiine-2, 2-dioxides (1), 2,3,4,5-tetra- hydrobenzothiepine-3, 5-dione-l,1-dioxides (2), 4-hydroxy-2- pyrones (3) 2, 4, 6-(1H,3H,5H)-pyrimidinetriones(4), tetronic acids (5) and 1, 2-oxathiolane-4-one-2, 2-dioxides (6) have been synthezised to examine structure activity relationships in the field of oral anticoagulants. The compounds are substituted by 4-chlorocinnamoyl, 1-phenylpropyl or l-(4-chlorophenyl)-3-oxo-butyl residues (R)in a suitable position. After single oral administration to rats (25-300 mg•kg-1) prothrombin levels (PT) of less than 25 percent are achieved within 10-48 hours with compounds of type 1-3 and 5. Compound of type 4 and 6 were inactive. The results show that not only 4-hydroxycoumarines (7) and 1,3-indanediones (8) exhibit indirekt anticoagulant activity. The lactone moiety of 7 can be replaced by a sultone moiety. The benzene ring needs not to be fused to the heterocyclic part of the molecule (see 3). The heterocyclic part may be a simple five memberea lactone. The effects of 8 can be extended to seven membered and even heterocyclic ring systems. Furthermore seme 2 showed platelet aggregation inhibiting activities (Born, IC50 = 5 • 10-4M). Some 5 showed direct anticoagulant activity (PT, PTT, in vitro).

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