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A selective small molecule glucagon-like peptide-1 secretagogue acting via depolarization-coupled Ca(2+) influx.
Glucagon-like peptide-1 (GLP-1) is an incretin hormone that potentiates insulin secretion in a glucose-dependent manner. Selective GLP-1 secretagogue would be one of the potential therapeutic targetsExpand
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Linear peptide ETA antagonists: rational design and practical derivatization of N-terminal amino- and imino-carbonylated tripeptide derivatives☆
Abstract Novel linear tripeptides possessing high endothelin antagonist activity were derived from endothelin antagonistic cyclic pentapeptides represented by BQ-123. The N-terminal urea moiety ofExpand
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6-Carboxy-5,7-diarylcyclopenteno[1,2-b]pyridine derivatives: a novel class of endothelin receptor antagonists.
Compounds (2-5) with a 6-carboxy-5,7-diarylcyclopentenopyridine skeleton were designed, synthesized, and identified as a new class of potent non-peptide endothelin receptor antagonists. TheExpand
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5-Fluorouracil derivatives. XI. Synthesis of 1-hexylcarbamoyl-5-fluorouracil metabolites.
Main metabolites of 1-hexylcarbamoyl-5-fluorouracil, i.e., 1-(5-carboxypentylcarbamoyl)-, 1-(3-carboxypropylcarbamoyl)-, 1-(5-hydroxyhexylcarbamoyl)- and 1-(5-oxohexylcarbamoyl)-5-fluorouracils, wereExpand
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5-Fluorouracil Derivatives. XII. Synthesis and Antitumor Activity of α-Alkylthiomethyl-, α-Alkylsulfinylmethyl-, α-Alkylsulfonylmethyl-, andα-Acylthiomethyl-5-fluorouracils
For the purpose of diminishing the toxicity of 5-fluorouracil (1) and obtaining biologically active derivatives of 1 suitable for oral administration, alkylthiomethyl, alkylsulfinylmethyl,Expand
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Preparation of Potentially Antitumor-Active Vinyl Polymers Having 5-Fluorouracil Unit as a Component
Preparation et copolymerisation radicalaire de l'acrylate et du methacrylate de fluoro-5 uracite-1 methyle avec l'acrylate de methyle, l'acide methacrylique, l'acrylonitrile, l'acide acrylique, leExpand
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A NEW SYNTHETIC ROUTE OF β-HYDROXYALKYLPHOSPHONATES FROM β,γ-EPOXYALKYLPHOSPHONATES
β-Hydroxyalkylphosphonates were synthesized from β,γ -epoxyalkylphosphonates and RMgX/ cat. CuI reagents, which is a new synthetic route for the various types of α- and/or γ-substitutedExpand
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Structure-Activity relationships of 2-substituted 5,7-Diarylcyclopenteno[1,2-b]pyridine-6-carboxylic acids as a novel class of endothelin receptor antagonists.
Synthesis and structure-activity relationships of 2-substituted-5,7-diarylcyclopenteno[1,2-b]pyridine-6-carboxylic acids, a novel class of endothelin receptor antagonists, were described.Expand
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