1027282-01-4Relevant academic research and scientific papers
Development of a Novel Series of Trialkoxyaryl Derivatives as Specific and Competitive Antagonists of Platelet Activating Factor
Sawyer, David A.,Beams, Richard M.,Blackwell, Geoffrey, J.,Brockwell, Michael A.,Cheesman, Neil J.,et al.
, p. 2130 - 2137 (2007/10/02)
The synthesis and structure-activity relationship (SAR) analysis of a novel series of trialkoxyaryl derivatives as specific and competetive inhibitors of platelet activating factor (PAF), are described.Molecular modeling comparisons of PAF with the known antagonists Ginkgolide B and L-652731 led to the selection of N-ethyl>-N,N,N-trimethylammonium iodide (1) from the Wellcome registry of compounds and to the synthesis of the lead compound N-oxy>ethyl>-N,N,N-trimethylammonium iodide (3, pKb 5.43).Furth er SAR considerations directed the design to 2-(hexyloxy)-1,3-dimethoxy-5-benzene (38) (pKb 7.14), a novel, specific, and competitive inhibitor of the PAF receptor in rabbit-washed platelets.
