Novel phomactin analogues as PAF receptor ligands

William P D Goldring; Stephen P H Alexander; David A Kendall; Gerald Pattenden

doi:10.1016/j.bmcl.2005.04.048

Novel phomactin analogues as PAF receptor ligands

Bioorg Med Chem Lett. 2005 Jul 1;15(13):3263-6. doi: 10.1016/j.bmcl.2005.04.048.

Authors

William P D Goldring¹, Stephen P H Alexander, David A Kendall, Gerald Pattenden

Affiliation

¹ School of Chemistry, The University of Nottingham, University Park, Nottingham NG7 2RD, UK.

PMID: 15922596
DOI: 10.1016/j.bmcl.2005.04.048

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Blood Platelets
Cell Membrane / chemistry
Heterocyclic Compounds, 4 or More Rings / chemical synthesis*
Heterocyclic Compounds, 4 or More Rings / pharmacology
Humans
Inhibitory Concentration 50
Ligands
Platelet Activating Factor / antagonists & inhibitors*
Platelet Membrane Glycoproteins / chemistry*
Platelet Membrane Glycoproteins / isolation & purification
Receptors, G-Protein-Coupled / chemistry*
Receptors, G-Protein-Coupled / isolation & purification
Structure-Activity Relationship

Substances

Heterocyclic Compounds, 4 or More Rings
Ligands
Platelet Activating Factor
Platelet Membrane Glycoproteins
Receptors, G-Protein-Coupled
platelet activating factor receptor
phomactin A