Preparation and pharmacological evaluation of 4-(1,4-benzoquinon-2-yl)-4-phenylbutanamides as potential cerebral protective agents.
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.
Tatsuoka
T
T
Suntory Institute for Biomedical Research, Osaka, Japan.
Suzuki
K
K
Imao
K
K
Satoh
F
F
Ishihara
T
T
Hirotsu
I
I
Kihara
T
T
Hatta
M
M
Horikawa
Y
Y
Sumoto
K
K
D000818:Animals; D016227:Benzoquinones / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D002317:Cardiovascular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002534:Hypoxia, Brain / Q000517:prevention & control*; D066298:In Vitro Techniques; D015227:Lipid Peroxidation / Q000187:drug effects; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D051381:Rats; D017208:Rats, Wistar
D016227:Benzoquinones; D002317:Cardiovascular Agents