Preparation and pharmacological evaluation of 4-(1,4-benzoquinon-2-yl)-4-phenylbutanamides as potential cerebral protective agents. |
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Authors: | T Tatsuoka K Suzuki K Imao F Satoh T Ishihara I Hirotsu T Kihara M Hatta Y Horikawa K Sumoto |
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Institution: | Suntory Institute for Biomedical Research, Osaka, Japan. |
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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 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. |
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