Synthesis, toxicological and pharmacological assessment of morpholinooximes.
The synthesis, pharmacology and toxicology of four morpholine derivatives from 1-(2-arylmorpholino)-3-phenyl-3-propanonoxime and the synthesis of two anilides are described. The structures of the synthesized derivatives were proved by IR, 1H NMR and occasionally with 13C NMR. The acute toxicity of the compounds in mice was determined. A comparative pharmacological study of the in vivo effect on the central nervous system was realised by the following screening tests: pentobarbital induced sleeping time, locomotor activity and behaviour despair test for antidepressive activity. The most active compound was 1-(2-phenylmorpholino)-3-phenyl-3-propanonoxime (2b) which showed low toxicity and antidepressive activity at a dose of 1/10 LD50.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sofia, Bulgaria.
P D
PD
Avramova
N D
ND
Danchev
R T
RT
Buyukliev
D000818:Animals; D000928:Antidepressive Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009025:Morpholines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D009043:Motor Activity / Q000187:drug effects; D010091:Oximes / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D010424:Pentobarbital / Q000494:pharmacology; D012890:Sleep / Q000187:drug effects; D013997:Time Factors
C120869:1-(2-phenylmorpholino)-3-phenyl-3-propanonoxime; D000928:Antidepressive Agents; D009025:Morpholines; D010091:Oximes; D010424:Pentobarbital