90857-77-5Relevant articles and documents
Analogues of Platelet Activating Factor. 6. Mono- and Bis-Aryl Phosphate Antagonists of Platelet Activating Factor
Wissner, A.,Carroll, M. L.,Green, K. E.,Kerwar, S. S.,Pickett, W. C.,et al.
, p. 1650 - 1662 (2007/10/02)
A series of aryl phosphoglyceride (3, 19-61) and bis-aryl phosphate (67-135) antagonists of platelet activating factor (PAF) were prepared.A group of four bifunctional phosphorus reagents (5a-c and 7) were developed that allowed the preparation of these aryl phosphates in which the position of aromatic substitution can be varied.These compounds were examined for their ability to inhibit PAF-induced platelet aggregation of rabbit platelets.Selected compounds were also evaluated for their ability to displace PAF from its receptor on 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 both the mouse and rabbit, 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.Compound 105 (CL 184005) has been selected to undergo further development as a potential therapeutic agent for the treatment of septic shock in man.
Phosphocholine derivatives having antihypertensive action
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, (2008/06/13)
Phosphocholine derivatives and compositions are described which are useful as hypotensive agents and in the treatment of hypertension in warm-blooded animals.
Analogues of platelet activating factor (PAF). I. Some modifications of the alkoxy chain
Wissner,Sum,Schaub,Kohler,Goldstein
, p. 1174 - 1181 (2007/10/02)
Analogues of platelet activating factor (PAF) in which the ether oxygen has been removed and in which the alkoxy chain at C1 has been replaced with a o-, p-, or m-alkylphenoxy group (30, 31, and 35, respectively) have been prepared. Compound 6 shows reduced platelet aggregation and hypotensive activity in comparison with C16 and C18 PAF. The results obtained for compounds 30, 31, and 35 indicate that the hypotensive and platelet aggregating responses are sensitive to structural modification of the ether chain. The ortho analogue 30 shows no platelet aggregating activity and only a weak hypotensive response. The para analogue 31 exhibits a moderate decrease in activity in both assays. The meta analogue 35 is the most active of the three.