Pyrimidine derivatives. 4. Synthesis and antihypertensive activity of 4-amino-2-(4-cinnamoylpiperazino)-6,7-dimethoxyquinazoline derivatives

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Abstract
A series of 30 4-amino-2-(4-cinnamoylpiperazino)-6,7-dimethoxyquinazoline derivatives was prepared and tested for their ability to reduce blood pressure in conscious, spontaneously hypertensive rates (SHR). The 4-amino-2-(4-cinnamoylpiperazino)-6,7-dimethoxyquinazolines 3a [4-amino-2-(4-cinnamoylpiperazino)-6,7-dimethoxyquinazoline hydrochoride] (R1 = H; R2 = Ph) and 3j [4-amino-2-[4-(4-ethoxycinnamoyl)piperazino]-6,7-dimethoxyquinazoline] (R1 = H; R2 = 4-EtOPh) showed activity at oral doses of 0.3-10 mg/kg. The effects of the 4-substituents of the piperazino group on activity are discussed. Compounds 3a and 3i were effective in renal hypertensive rats at oral doses of 3 and 10 mg/kg, and showed .alpha.-adrenoceptor blocking effects in isolated aortas of rats. A 5-day consecutive oral administration of 3a and 3j in SHR did not lead to development of tolerance.

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