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Preparation and pharmacological evaluation of 4-(1,4-benzoquinon-2-yl)-4-phenylbutanamides as potential cerebral protective agents.
Authors:T Tatsuoka  K Suzuki  K Imao  F Satoh  T Ishihara  I Hirotsu  T Kihara  M Hatta  Y Horikawa  K Sumoto
Institution:Suntory Institute for Biomedical Research, Osaka, Japan.
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 synthesized showed significant antilipidperoxidation (ALP) activities with brain homogenate in rats and some of them possessed a protective effect against hypobaric hypoxia in mice. Especially, a thiomorpholine derivative (2l, 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.
Keywords:
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