Studies on Cardiotonic Agents. V. Synthesis of 1-(6, 7-Dimethoxy-4-quinazolinyl)piperidine Derivatives Carrying Various 5-Membered Heterocyclic Rings at the 4-Position

Yuji NOMOTO; Haruki TAKAI; Tadashi HIRATA; Masayuki TERANISHI; Tetsuji OHNO; Kazuhiro KUBO

doi:10.1248/cpb.39.86

Yuji NOMOTO, Haruki TAKAI, Tadashi HIRATA, Masayuki TERANISHI, Tetsuji OHNO, Kazuhiro KUBO

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Keywords: cardiotonic agent, structure-activity relationship, piperidine, quinazoline, 3-amino-4-oxo-2-thioxoimidazolidine, 2, 4-dihydro-3-thioxo-3H-1, 2, 4-triazole, 2, 4-dihydro-3-oxo-3H-pyrazole, 5-amino-2, 3-dihydro-2-thioxo-3H-1, 3, 4-thiadiazole

JOURNAL FREE ACCESS

1991 Volume 39 Issue 1 Pages 86-90

DOI https://doi.org/10.1248/cpb.39.86

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Abstract

A series of 1-(6, 7-dimethoxy-4-quinazolinyl)piperidines carrying various 5-membered heterocycles at the 4-position was synthesized and examined for cardiotonic activity in anesthesized dogs. The (4-oxo-2-thioxo-3-imidazolidinyl)amino derivatives showed the most potent inotropic activity. Marked loss of activity was observed in the 2, 4-dihydro-3-thioxo-3H-1, 2, 4-triazolyl, the 2, 4-dihydro-3-oxo-3H-pyrazolyl and the (2, 3-dihydro-2-thioxo-3H-1, 3, 4-thiadiazol-5-yl)amino derivatives. The synthesis and structure-activity relationships are discussed.

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