Synthesis and pharmacological evaluation of 1,2,3,4-tetrahydro-beta-carboline derivatives.
A series of 1,2,3,4-tetrahydro-beta-carbolines has been synthesized and evaluated for cerebral protecting effects against lipid peroxidation and potassium cyanide intoxication in mice. Most of the compounds synthesized had potent effects against lipid peroxidation. Among them, 1-(3,5-dimethoxyphenyl)-2-propyl-1,2,3,4-tetrahydro-beta-carboline (22) was found to have a combination of potent effects against both lipid peroxidation and potassium cyanide intoxication. Structure-activity relationships are discussed.
Kawashima
Y
Y
Research Center, Taisho Pharmaceutical Co., Ltd., Saitama, Japan.
Horiguchi
A
A
Taguchi
M
M
Tuyuki
Y
Y
Karasawa
Y
Y
Araki
H
H
Hatayama
K
K
D000818:Animals; D001927:Brain Diseases / Q000378:metabolism / Q000517:prevention & control; D002243:Carbolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D000860:Hypoxia / Q000188:drug therapy / Q000378:metabolism; D015227:Lipid Peroxidation / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D018696:Neuroprotective Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D011190:Potassium Cyanide / Q000506:poisoning; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
D002243:Carbolines; D018696:Neuroprotective Agents; D011190:Potassium Cyanide