123546-46-3Relevant academic research and scientific papers
2,4-disubstituted derivatives of tetrahydrofuran useful for the treatment of PAF mediated illnesses
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, (2008/06/13)
The present invention describes novel 2,4-disubstituted derivatives of tetrahydrofuran, having the formula I STR1 wherein: -X- is either an oxygen atom or a covalent single bond; --CH2 XR1 group is in the position 2 and --CH2 OR2 is in the position 4 of the tetrahydrofuran ring, or --CH2 XR1 is in position 4 and --CH2 OR2 in position 2; -R1 represents an alkyl or an alkylaminocarbonyl group; -R2 represents a group having the formula -Y-(CH2)n -Q.(A-)q where -Y- is a covalent single bond, a carbonyl group, a carbonyloxy group or a carbonylamino group; n is an integer 0 to 10; Q is a nitrogen containing heterocycle; q is one when Q is charged or q zero when Q is neutral; and A- is a pharmaceutically acceptable anion. These compounds are PAF antagonists and, thus, useful for the treatment of diseases in which PAF is involved.
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.
