Synthesis of 1- and 3-(1-substituted 4-piperidinyl)-1,2,3,4-tetrahydro-2-oxoquinazolines as potential antihypertensive agents

DOI: 10.1248/cpb.33.1116

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 1116 - 1128 (1985)

Update date:2022-09-26

Topics:

Authors:

Takai Takai

Obase Obase

Nakamizo

Teranishi

Kubo Kubo

Shuto Shuto

Kasuya Kasuya

Shigenobu

Hashikami

Karashima

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Article abstract of DOI:10.1248/cpb.33.1116

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 (KF5908) seemed the most promising.

Full text of DOI:10.1248/cpb.33.1116

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