Journal of Medicinal Chemistry p. 382 - 389 (1981)
Update date:2022-08-04
Topics:
Bennett, Lawrence R.
Blankley, C. John
Fleming, Robert W.
Smith, Ronald D.
Tessman, Deirdre K.
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.
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