Synthesis and Evaluation of Novel Pyrazolo[1,5-a]pyrimidine Derivatives as Nonpeptide Angiotensin II Receptor Antagonists

概要

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A novel series of 6-alkyl-7-oxo-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carboxylic acid derivatives was prepared as angiotensin II (AII) receptor antagonists. When evaluated in an in vitro binding assay using COS cells transfected with a cDNA encoding a human AT_1 angiotensin II receptor, the compounds in this series showed K_i values in the range of 0.4-4.0 nM. In anesthetized spontaneously hypertensive rats (SHRs), administration of the 6-propyl derivative 4d (1 mg/kg, i.v.) reduced the mean blood pressure (MBP) by a maximum of more than 30 mmHg from the normal value.
社団法人日本薬学会の論文
1995-06-15