5660-49-1Relevant academic research and scientific papers
Aminoacylates and aminocarbamates of 2-substituted 4-hydroxymethyl 1,3-dioxolans as ammonium salts. A new series of PAF antagonists
Broquet, C,Auclair, E,Blavet, N,Touvay, C,Braquet, P
, p. 235 - 240 (1990)
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.
Disubstituted tetrahydrofurans and dioxolanes as PAF antagonists
Bartroli,Carceller,Merlos,Garcia-Rafanell,Forn
, p. 373 - 386 (2007/10/02)
A new series of disubstituted tetrahydrofuran and dioxolane derivatives were prepared and evaluated for their PAF antagonist activity in the PAF-induced in vitro platelet-aggregation and in vivo hypotension tests. Several of these compounds exhibited more potent activity than the structurally related 2-[N-acetyl-N-[[[[2-methoxy-3-[(octadecylcarbamoyl)oxy]propoxy] carbonyl]amino]methyl]-1-ethylpyridinium chloride (CV-6209, 3) in the in vitro assay, whereas all showed less potency in the in vivo test. The role of both the substituent nature and the placement and number of oxygen atoms in the ring are discussed. A qualitative SAR study was carried out on these nuclei.
New 1,3-dioxolan-4-yl derivatives of 2-picolylamine
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, (2008/06/13)
The present invention relates to new 1,3-dioxolan-4-yl derivatives of 2-picolylamine having the formula (I): wherein:, R1 represents an alkyl or phenylalkyl radical; R2 represents hydrogen, C1-C4--acyl or C
