Aminoacylates and aminocarbamates of 2-substituted 4-hydroxymethyl 1,3-dioxolans as ammonium salts. A new series of PAF antagonists

Article abstract of DOI:10.1016/0223-5234(90)90206-I

The synthesis and biological activity of some aminoacylate and aminocarbamate ammonium salts of 2-substituted 4-hydroxymethyl 1,3-dioxolans are described.The compounds were obtained as mixtures of diastereoisomeric racemates.In vitro, platelet aggregation (PPR) induced by PAF was antagonized by all derivatives.In vivo (in the guinea pig, iv), the PAF-induced bronchoconstriction, thrombocytopenia and leukopenia, were inhibited by most of them.Among the synthesized compounds, two highly potent and specific PAF antagonists: BN 52111 and BN 52115 have been identified.