Preparation and Pharmacological Evaluation of 4-(1, 4-Benzpouinon-2-yl)-4-phenylbutanamides as Potantial Cerebral Protective Agents1)

Toshio TATSUOKA; Kenji SUZUKI; Kayoko IMAO; Fumio SATOH; Takehumi ISIHARA; Ichiro HIROTU; Tetsuro KIHARA; Mizuho HATTA; Yoshiko HORIKAWA; Kunihiro SUMOTO; Seiji MIYANO

doi:10.1248/cpb.40.2382

Preparation and Pharmacological Evaluation of 4-(1, 4-Benzpouinon-2-yl)-4-phenylbutanamides as Potantial Cerebral Protective Agents¹)

Toshio TATSUOKA, Kenji SUZUKI, Kayoko IMAO, Fumio SATOH, Takehumi ISIHARA, Ichiro HIROTU, Tetsuro KIHARA, Mizuho HATTA, Yoshiko HORIKAWA, Kunihiro SUMOTO, Seiji MIYANO

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Keywords: SUN-4757, 2, 3, 4, 5-tetrahydro-1-benzoxepin-2-one, 4-phenylbutanamide, 1, 4-benzoquinone, N-substituted thiomorpholine, antilipidperoxidation, cerevral protective agent

JOURNAL FREE ACCESS

1992 Volume 40 Issue 9 Pages 2382-2386

DOI https://doi.org/10.1248/cpb.40.2382

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Abstract

A new series of 4-(1, 4-benzoquinon-2-yl)-4-phenylbutanamides (2) were synthesized for evaluation of their pharmacological activities. All these compounds sythesized showed singnificant antilipidperoxidation (ALP) activities with brain homogenate in rats and some of them possessed a protective effect against hypobaric hypoxia in mice.Especially, a thiomopholine derivative (21, SUN-4757) showed a wide efficacy spectrum to a variety of experimental screening assays designed for cerebral protective agents, and it had a high LD₅₀ value.

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