Preliminary pharmacological evaluation of newly synthesized derivatives of phosphonoamino acids.

Ten newly synthesized derivatives of phosphonoamino acids were subjected to preliminary pharmacological evaluation in mice and rats. We investigated their effect on acute toxicity, body temperature, spontaneous and exploratory activity, electrogenic and pentetrazole convulsions, and motor coordination and gamma-amino-butyric acid concentration in various brain regions. The most active derivatives were alpha-amino-alpha-p-hydroxyphenyl-methylphosphonic acid 40, beta-(alpha-aminoethyl)-carbamoyl-ethylphosphonic acid 43, alpha-amino-beta-phenylethylphosphonic acid 46, and alpha-amino-beta-(p-nitrophenyl)-ethylphosphonic acid 47. Those compounds depressed the spontaneous locomotor activity and displayed protective action in electrogenic and pentetrazole convulsions.