Synthesis of 1-and 3-(1-Substituted 4-Piperidinyl)-1, 2, 3, 4-tetrahydro-2-oxoquinazolines as Potential Antihypertensive Agents

Abstract

A series of 1-and 3-(1-substituted 4-piperidinyl)-1, 2, 3, 4-tetrahydro-2-oxoquinazolines were synthesized and tested for antihypertensive activity. Among the compounds tested, 1-(2-hydroxy-2-phenethyl)-4-(1, 2, 3, 4-tetrahydro-2-oxo-3-quinazolinyl) piperidine derivatives were generally the most effective in lowering blood pressure in the spontaneous hypertensive rat model. Of these, 1-[2-(4-chlorophenyl)-2-hydroxyethyl]-4-(1, 2, 3, 4-tetrahydro-2-oxo-3-quinazolinyl) piperidine (26) (KF5908) seemed the most promising.