ABSTRACT
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.
Subject(s)
Antidepressive Agents/chemical synthesis , Morpholines/chemical synthesis , Oximes/chemical synthesis , Animals , Antidepressive Agents/pharmacology , Antidepressive Agents/toxicity , Lethal Dose 50 , Male , Mice , Morpholines/pharmacology , Morpholines/toxicity , Motor Activity/drug effects , Oximes/pharmacology , Oximes/toxicity , Pentobarbital/pharmacology , Sleep/drug effects , Time FactorsABSTRACT
Complexes of La(III) with 1-aminocyclopentane-, -hexane, -heptane and -4-ethylcyclohexanecarboxylic acids were obtained. The compounds were characterized by elemental analyses, IR spectroscopy and conductivity measurements. The following general formula was derived: LaL3Cl3 x 5 H2O, where L is the corresponding 1-aminocycloalkanecarboxylic acid. The pharmacological studies showed that all complexes manifested higher cytostatic and cytotoxic effects in comparison with lanthanum chloride. Much higher cytotoxic (anti-P388/D1) and cytostatic (anti-L-1210 and anti-melanoma-B16) activity was found for the lanthanum complex with 1-aminocyclopentanecarboxylic acid.
