A Practical Synthesis of Optically Active Platelet-Activating Factor Antagonist, (+)-6-(2-Chlorophenyl)-3-cyclopropanecarbonyl-8,11-dimetyl-2,3,4,5-tetrahydro-8H-pyrido(4',3':4,5)thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepine(E6123), and Its Absolute Configuration.
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چکیده
منابع مشابه
SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF 6-CARBETHOXY-5-(3'-BROMOPHENYL)-3-ARYL-2-CYCLOHEXENONES AND 6-ARYL-4-(3'-BROMOPHENYL)-3-OXO-2,3A,4,5-TETRAHYDRO-2H-INDAZOLES
6-Carbethoxy-5-(3'-bromophenyl)-3-aryl-2-cyclohexenones 2a-j were obtained from the1-Aryl-3-(3'-bromophenyl)-2-propene-1-ones 1a-j by Micheal addition of ethyl acetoacetate, followed by internal Claisen condensation. Reaction of 2a-j with hydrazine hydrate afforded the corresponding 6-Aryl-4-(3'-bromophenyl)-3-oxo-2,3a,4,5-tetrahydro-2H-indazoles 3a-j. The structures of newly synthesized compou...
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Rupatadine (UR-12592, 8-chloro-6, 11-dihydro-11-[1-[(5-methyl3-pyridinyl) methyl]-4-piperidinylidene]-5H-benzo[5,6]-cyclohepta[1,2b]pyridine ) is a novel compound that inhibits both platelet-activating factor (PAF) and histamine (H1) effects through its interaction with specific receptors (Ki(app) values against [3H]WEB-2086 binding to rabbit platelet membranes and [3H]-pyrilamine binding to gu...
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15 صفحه اولEffect of platelet activating factor antagonist treatment on gentamicin nephrotoxicity
To assess whether PAF could be involved in the gentamicin-induced nephrotoxicity, we have studied the effect of PAF antagonist BN-52021 on renal function in rats after gentamicin (GENTA) treatment. Experiments were completed in 21 Wistar rats divided into three groups: group GENTA was injected with gentamicin 100 mg kg(-1) body wt/day s.c. for 6 days. Group GENTA + BN received gentamicin and BN...
متن کاملSynthesis of new optically active 2-pyrrolidinones.
A new class of optically active 2-pyrrolidinones was synthesized, starting from S-pyroglutamic acid, a well known natural chiral synthon. The synthetic design followed led to the insertion of various substituents at positions 1 and 5 of the 2-pyrrolidinone ring, including the imidazole moiety. Some of them possess two or three stereogenic centers, the configuration of which was retained under t...
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ژورنال
عنوان ژورنال: Chemical and Pharmaceutical Bulletin
سال: 1992
ISSN: 0009-2363,1347-5223
DOI: 10.1248/cpb.40.521