Document Report Card

ID: ALA1121810

Journal: J Med Chem

Title: Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives.

Authors: Bennett LR, Blankley CJ, Fleming RW, Smith RD, Tessman DK.

Abstract: A series of 51 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives was prepared and evaluated for antihypertensive activity in the conscious spontaneously hypertensive rat. A number of these compounds, notably 6-(2,6-dichlorophenyl)-2-methylpyrido[2,3-d]pyrimidin-7-amine (36), lowered blood pressure in these rats in a gradual and sustained manner to normotensive levels at oral doses of 10-50 mg/kg. Normalized blood pressure levels could then be maintained by single daily oral doses. The effect of structural variation in the 6-aryl group and in the 2 and 4 positions of the pyridopyrimidine ring on activity is reported and discussed.

CiteXplore: 7265125

DOI: 10.1021/jm00136a006