SYNTHESIS AND PAF ANTAGONIST ACTIVITY OF SOME 2,5-DIARYLTETRAHYDROFURANS INCORPORATING PAF-LIKE FUNCTIONAL-GROUPS

This paper describes the synthesis and structure-activity relationship s of a series of 2,5-diaryltetrahydrofurans, as specific and potent an tagonists at the rabbit washed platelet activating factor (PAF) recept or. The methoxyl groups in the known PAF antagonist L-652,731 were rep laced with functional groups present in PAF and in the 'PAF-like' anta gonists. Activity was generally retained or enhanced when one aryl rin g in L-652,731 was elaborated; however incorporation of these function al groups into both of the aryl rings greatly reduced or abolished act ivity. These results are discussed in relation to a putative model for the PAF receptor.