Synthesis and pharmacological properties of derivatives of alpha-amino-beta-(p-chlorobenzoyl)-propionic acid and alpha-amino-gamma-(p-chlorophenyl)-tetrahydrofuran-2-one.
Several new alpha-aminoderivatives of gamma-(p-chlorophenyl)-tetrahydrofuran-2-one were synthesized. alpha-Aminoderivatives of beta-(p-chlorobenzoyl)-propionic acid 2-13 were used as the substrates. After the reduction with NaBH4 at 10-12 degrees C and cyclization the compounds were converted into the appropriate derivatives of tetrahydrofuran-2-one 16-26. In pharmacological tests compounds 9 and 26 abolished the aggressiveness in isolated mice while compound 8 showed antiinflammatory activity.
Zabska
R
R
Department of Chemistry of Drug, Medical Academy, Wrocław, Poland.
Jakóbiec
T
T
Dobek
R
R
Wilimowski
M
M
Barczyńska
J
J
Kedzierska-Goździk
L
L
Wojewódzki
W
W
Rutkowska
M
M
Duś
E
E
Szelag
A
A
D000374:Aggression / Q000187:drug effects*; D000700:Analgesics / Q000494:pharmacology; D000818:Animals; D000893:Anti-Inflammatory Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D000927:Anticonvulsants / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects* / Q000502:physiology; D018492:Dopamine Antagonists; D005260:Female; D005663:Furans / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D051381:Rats; D011919:Rats, Inbred Strains; D012110:Reserpine / Q000037:antagonists & inhibitors; D012702:Serotonin Antagonists / Q000494:pharmacology; D013055:Spectrophotometry, Infrared
D000700:Analgesics; D000893:Anti-Inflammatory Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000927:Anticonvulsants; D018492:Dopamine Antagonists; D005663:Furans; D012702:Serotonin Antagonists; D012110:Reserpine