139907-03-2Relevant academic research and scientific papers
Analogues of platelet activating factor. 7. Bis-aryl amide and bis-aryl urea receptor antagonists of PAF
Wissner,Carroll,Johnson,Kerwar,Pickett,Schaub,Torley,Trova,Kohler
, p. 4779 - 4789 (2007/10/02)
A series of bis-aryl amide (13-57 and 66-81) and bis-aryl urea (58 and 85) antagonists of platelet-activating factor (PAF) was prepared that contain, separating the two aromatic rings, linear amide linkages of the form - (CH2)(n)CONH- (n = 0-2), -OCH2CONH-, and -(CH2)(n)NHCO- (n = 0-1), branched amide linkages of the form -(CH2)(n)N(COR)- (n = 1-3, R = CH3 or n-C3H7), and -N(COCH3)CH2-, and urea linkages of the form -NHCONH- and - CH2N(CONHCH3)-. These compounds were examined for their ability to inhibit PAF-induced platelet aggregation of rabbit platelets. These in vitro data were compared to similar data obtained for a number of known PAF antagonists. The compounds were evaluated in vivo, in the mouse, for their ability to prevent death induced by a lethal challenge of PAF. The relationships between the biological activity and the nature, lipophilicity, and position of substituents of the aromatic rings were studied. Best activity was observed for compounds having linkages of the type -CH2CONH-, -CH2N(COR)-, and - CH2NHCO-. Many of these compounds inhibit PAF-induced platelet aggregation with IC50's under 1 μM.
Bis-aryl amide and urea antagonists of platelet activating factor
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, (2008/06/13)
Bis-aryl amide and urea compounds of the general formula: STR1 wherein X is a divalent amide or urea substituent and Y is a nitrogen containing heterocycle, which compounds are inhibitors of platelet activating factor. Pharmaceutical compositions containing the compounds and methods of treating platelet activating factor associated conditions are also included.
Method of preparing bis-aryl amide and urea antagonists of platelet activating factor
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, (2008/06/13)
Methods of preparing bis-aryl amide and urea compounds of the general formula: STR1 wherein x is a divalent amide or urea substituent and Y is a nitrogen containing heterocycle, which compounds are inhibitors of platelet activating factor.
