Novel phomactin analogues as PAF receptor ligands.
A range of natural and unnatural phomactins, recently synthesised in our laboratory, were found to exhibit PAF antagonism with pIC(50) values in the range 5.6-6.2. The variation in structural and stereochemical features between the phomactins was found to have only a modest effect on the inhibition of binding of PAF to its human platelet receptors.
Goldring
William P D
WP
School of Chemistry, The University of Nottingham, University Park, Nottingham NG7 2RD, UK.
Alexander
Stephen P H
SP
Kendall
David A
DA
Pattenden
Gerald
G
D001792:Blood Platelets; D002462:Cell Membrane / Q000737:chemistry; D006576:Heterocyclic Compounds, 4 or More Rings / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D010972:Platelet Activating Factor / Q000037:antagonists & inhibitors*; D010980:Platelet Membrane Glycoproteins / Q000737:chemistry* / Q000302:isolation & purification; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry* / Q000302:isolation & purification; D013329:Structure-Activity Relationship
D006576:Heterocyclic Compounds, 4 or More Rings; D008024:Ligands; D010972:Platelet Activating Factor; D010980:Platelet Membrane Glycoproteins; D043562:Receptors, G-Protein-Coupled; C039351:platelet activating factor receptor; C413206:phomactin A