Preliminary pharmacological evaluation of newly synthesized derivatives of phosphonoamino acids
Kleinrok, Z.; Kolasa, K.; Mastalerz, P.; Kafarski, P.
Polish Journal of Pharmacology and Pharmacy 38(5-6): 435-442
1986
ISSN/ISBN: 0301-0244 PMID: 3575164 Document Number: 269105
Ten newly synthesized derivatives of phosphonoamino acids were subjected to preliminary pharmacological evaluation in mice and rats. We investigate their effect on acute toxicity, body temperature spontaneous and exploratory activity, electrogenic and pentetrazole convulsions, and motor coordination and .gamma.-aminobutyric as 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 penetetrazole convulsions.