Structure-Activity Relationship in PAF-acether. 4. Synthesis and Biological Activities of Carboxylate Isosteres

Article abstract of DOI:10.1021/jm00397a025

The synthesis and biological characterization of some 3-carboxylate isosteres of PAF-acether structurally modified in positions 1 (ether, carbamate), 2 (acetoyl, ethoxy), and 3 (chain length and polar head group) are reported.All derivatives present antagonist activities against PAF-acether-induced effects in vitro (platelet aggregation) and in vivo (bronchoconstriction and thrombocytopenia in guinea pig and, to a lesser extent, hypotension in rat).The functional modifications presented here do not modify dramatically the potency of antagonist activities, and there is no enantioselectivity.All of the isosteres are specific PAF-acether...