Platelet-activating factor (PAF) is a naturally occurring alkyl ether phospholipid that was first described by Benveniste in 1972. This substance was structurally identified 7 yr later. Over the years, a great deal of information has become available concerning the role of PAF in a number of pathological conditions like asthma, septic shock and gastric ulceration. Therefore, many laboratories have been engaged in research projects on the synthesis and development of PAF-antagonists, which may be useful in the treatment of these and other inflammatory diseases. In our study, we have prepared some new PAF-antagonists with the propyl backbone constrained in a more rigid structure, namely the 2-oxazolidinone and 2-morpholinone rings (compounds 13-16, 24-36 and 40). Their activity as PAF-antagonists on the inhibition of rabbit platelet aggregation was evaluated in comparison with the known antagonists with similar structures CV-3988, SRI-63441 and Ro-193704.
New antagonists of platelet-activating factor containing 2-oxazolidinone or 2-morpholinone.
ABELLI, Luigi;
1994
Abstract
Platelet-activating factor (PAF) is a naturally occurring alkyl ether phospholipid that was first described by Benveniste in 1972. This substance was structurally identified 7 yr later. Over the years, a great deal of information has become available concerning the role of PAF in a number of pathological conditions like asthma, septic shock and gastric ulceration. Therefore, many laboratories have been engaged in research projects on the synthesis and development of PAF-antagonists, which may be useful in the treatment of these and other inflammatory diseases. In our study, we have prepared some new PAF-antagonists with the propyl backbone constrained in a more rigid structure, namely the 2-oxazolidinone and 2-morpholinone rings (compounds 13-16, 24-36 and 40). Their activity as PAF-antagonists on the inhibition of rabbit platelet aggregation was evaluated in comparison with the known antagonists with similar structures CV-3988, SRI-63441 and Ro-193704.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
