Studies on 2-oxoquinoline derivatives as blood platelet aggregation inhibitors. II. 6-(3-(1-Cyclohexyl-5-tetrazolyl)propoxy)-1,2-dihydro-2-oxoquinoline and related compounds. - Concepedia

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Studies on 2-oxoquinoline derivatives as blood platelet aggregation inhibitors. II. 6-(3-(1-Cyclohexyl-5-tetrazolyl)propoxy)-1,2-dihydro-2-oxoquinoline and related compounds.

DOI Full Paper Access

60

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0

References

1983

Year

Takao Nishi, Fujio Tabusa, Tatsuyoshi Tanaka, Takefumi Shimizu, Toshimi Kanbe, Yukio Kimura, KAZUYUKI NAKAGAWA

Chemical and Pharmaceutical Bulletin

Pharmaceutical ScienceBioorganic ChemistryCollagen-and Adenosine DiphosphatePharmacotherapyRelated CompoundsPharmaceutical ChemistryThrombosisMolecular PharmacologyMedicinal ChemistryHematologyPlatelet AntagonistInhibitory ActivityRabbit Blood PlateletsBiochemistryPharmacological AgentPharmacology2-Oxoquinoline DerivativesBiomolecular EngineeringThrombopoiesisPlatelet Aggregation InhibitorsBlood PlateletNatural SciencesClinical PharmacologyMedicineAnticoagulantDrug Discovery

Abstract

A series of ω-(1-substituted-5-tetrazolylalkoxy)-2-oxoquinolines was synthesized and tested for inhibitory activity towards collagen-and adenosine diphosphate (ADP)-induced aggregation of rabbit blood platelets in vitro. These compounds were prepared by the reaction of 1-substituted-5-(ω-chloroalkyl)-tetrazoles and hydroxy-2-oxoquinolines in the presence of a base. Among them, 6-[3-(1-cyclohexyl-5-tetrazolyl)propoxy]-1, 2-dihydro-2-oxoquinoline (IVb) was found to have the most potent inhibitory activity. The structure-activity relationships are discussed.