Disubstituted tetrahydrofurans and dioxolanes as PAF antagonists
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.
Bartroli,Carceller,Merlos,Garcia-Rafanell,Forn
p. 373 - 386
(2007/10/02)
New 1,3-dioxolane-2-yl derivatives of 2-picolylamine
The present invention relates to new 1,3-dioxolan-2-yl derivatives of 2-picolylamine having the formula (I): wherein:, R1 represents an alkyl radical; R2 represents hydrogen, or a C(=O)R4 group, wherein R4 repre
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(2008/06/13)
1,y Dihydroxy paraffins
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Akal Baser
p. 524 - 526
(2007/10/05)
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