Abstract
In an effort to determine the effect of modification of the imidazo[2,1-a]isoquinoline portion of the PAF-receptor antagonist SDZ 64-412 (1), several new analogs were prepared and evaluated in vitro and in vivo. One of these, 5-[4-[2-(3,4,5-trimethoxyphenyl)ethyl]phenyl]-2,3-dihydroimidazo [1,2-a]thieno[2,3-c]pyridine (6) was 4-5 times more potent than 1 in inhibiting PAF-induced bronchoconstriction and hemoconcentration when administered po to the guinea pig.
MeSH terms
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Animals
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Binding, Competitive
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Bronchoconstriction / drug effects
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Guinea Pigs
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Humans
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Isoquinolines / chemical synthesis
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Isoquinolines / pharmacology*
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Platelet Activating Factor / antagonists & inhibitors*
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Platelet Membrane Glycoproteins / antagonists & inhibitors*
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Platelet Membrane Glycoproteins / metabolism
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Pyridines / chemical synthesis
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Pyridines / pharmacology*
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Receptors, Cell Surface*
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Receptors, G-Protein-Coupled*
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Structure-Activity Relationship
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Thienopyridines
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Thiophenes / chemical synthesis
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Thiophenes / pharmacology*
Substances
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5-(4-(2-(3,4,5-trimethoxyphenyl)ethyl)phenyl)-2,3-dihydroimidazo(1,2a)thieno(2,3-c)pyridine
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Isoquinolines
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Platelet Activating Factor
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Platelet Membrane Glycoproteins
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Pyridines
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Receptors, Cell Surface
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Receptors, G-Protein-Coupled
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Thienopyridines
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Thiophenes
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platelet activating factor receptor
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SDZ 64-412