[Synthesis of 1-trans-cinnamoyl- and 1-[trans-3-(pyridyl)acryloyl]-2-pyrrolidinone derivatives and their effect on hemicholinium-induced impairment of water maze learning in mice].
Various 1-trans-cinnamoyl-2-pyrrolidinones (6a-k) and 1-[trans-3-(pyridyl)acryloyl]-2-pyrrolidinones (9a-c) were prepared as analogues of the notropic agent, aniracetam (2), and their effects on hemicholinium-induced impairment of water maze learning in mice were examined. 1-(trans-3-Methoxycinnamoyl)-, 1-(trans-4-methoxycinnamoyl)- and 1-(trans-4-chlorocinnamoyl)-2-pyrrolidinones (6c, d, h) and 1-[trans-3-(3-pyridyl)acryloyl]-2-pyrrolidinone (9c) were found to be more active than aniracetam in these tests. In addition, these 2-pyrrolidinones (6a-k, 9a-c) were apparently observed to lengthen mouse survival time following hemicholinium injection into the brain.
Nagasaka
T
T
Tokyo College of Pharmacy, Japan.
Momose
K
K
Hamaguchi
F
F
Yamada
K
K
Yamada
H
H
Suzuki
Y
Y
D000818:Animals; D006426:Hemicholinium 3; D007859:Learning Disabilities / Q000139:chemically induced / Q000188:drug therapy*; D008297:Male; D051379:Mice; D011619:Psychotropic Drugs / Q000138:chemical synthesis* / Q000627:therapeutic use; D011760:Pyrrolidinones / Q000138:chemical synthesis* / Q000627:therapeutic use
C076427:1-(3-(3-pyridyl)acryloyl)-2-pyrrolidinone; C076425:1-(trans-3-(2-pyridyl)acryloyl)-2-pyrrolidinone; C076430:1-(trans-3-(4-pyridyl)acryloyl)-2-pyrrolidinone; D011619:Psychotropic Drugs; D011760:Pyrrolidinones; D006426:Hemicholinium 3