Abstract
Compounds 1 or 2 which possess dual-acting PAF antagonist/TxSI in a previous paper were modified and evaluated for the dual-acting activity. It was found that several compounds were potent dual-acting PAF antagonist/TxSI in and ex vivo. 6-(2-Chlorophenyl)-3-[4-[(E/Z)-6-ethoxycarbonyl-1-(3-pyridyl)-1-hexenyl]phenylmethyl]-8,11-dimethyl-2,3,4,5-tetrahydro-8H-pyrido[4',3': 4,5]thieno[3,2-f]triazolo[4,3-a]diazepine (12) is excellent orally dual-acting PAF antagonist/TxSI.
MeSH terms
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Animals
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Azepines / chemical synthesis*
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Azepines / chemistry
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Azepines / pharmacology*
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology*
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Platelet Aggregation / drug effects
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Platelet Aggregation Inhibitors / chemical synthesis
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Platelet Aggregation Inhibitors / pharmacology
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Platelet Membrane Glycoproteins / antagonists & inhibitors*
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Rats
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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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Thiophenes / chemical synthesis*
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Thiophenes / chemistry
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Thiophenes / pharmacology*
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Thromboxane-A Synthase / antagonists & inhibitors*
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Thromboxane-A Synthase / chemistry
Substances
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6-(2-chlorophenyl)-3-(4-(6-ethoxycarbonyl-1-(3-pyridyl)-1-hexenyl)phenyllmethyl)-8,11-dimethyl-2,3,4,5-tetrahydro-8H-pyrido(4',3'-4,5)thieno(3,2-f)(1,2,4)triazolo(4,3-a)diazepine
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Azepines
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Enzyme Inhibitors
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Platelet Aggregation Inhibitors
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Platelet Membrane Glycoproteins
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Receptors, Cell Surface
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Receptors, G-Protein-Coupled
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Thiophenes
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platelet activating factor receptor
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Thromboxane-A Synthase