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Endothelin antagonistic peptide derivatives with high selectivity for ETA receptors
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 targets… Expand
Endothelin antagonistic cyclic pentapeptides with high selectivity for ETA receptor
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 of… Expand
6-Carboxy-5,7-diarylcyclopenteno[1,2-b]pyridine derivatives: a novel class of endothelin receptor antagonists.
- K. Niiyama, T. Mase, +13 authors K. Ishikawa
- Medicine, Chemistry
- Bioorganic & medicinal chemistry
- 1 August 2002
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. The… Expand
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, were… Expand
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
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, le… Expand
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-substituted… Expand
Structure-Activity relationships of 2-substituted 5,7-Diarylcyclopenteno[1,2-b]pyridine-6-carboxylic acids as a novel class of endothelin receptor antagonists.
- K. Niiyama, Hirobumi Takahashi, +10 authors K. Ishikawa
- Medicine, Chemistry
- Bioorganic & medicinal chemistry letters
- 4 November 2002
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