[Synthesis and bioactivity of substituted alpha-aminobenzylphosphonate].
OBJECTIVE
To search for some substituted alpha-amino phosphonates as leading compounds with the vasodilator effects.


METHODS
Target compounds were prepared from benzyl aldehyde, piperazine and diethyl phosphite using alcohol as solvent via Mannich-type reaction. In isolated rat aorta and in isolated guinea pig ileum, the vasodilator effects of compounds were investigated and evaluated whether they activated muscarine receptor.


RESULTS
Seven compounds of substituted alpha-amino phosphonates have been synthesized and identified by IR, 1H NMR and elemental analysis. Three of them, compound 2a, 2b and 2c have vasodilator activity and do not activate M receptor.


CONCLUSIONS
Two (2b and 2c) of them were found to have the notable vasodilator effect, and the rates of relaxing are (67 +/- 21) % and (82 +/- 18)%, separately. But they did not activate M receptors on ileum.
Zhao
Li-zhi
LZ
Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing, China.
Yang
Ri-fang
RF
Zhao
Ru-sheng
RS
Zhang
Yan-fang
YF
Chen
Dong-mei
DM
Wang
Hai
H
D000818:Animals; D001011:Aorta / Q000187:drug effects; D001596:Benzylamines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D015394:Molecular Structure; D009119:Muscle Contraction / Q000187:drug effects*; D063065:Organophosphonates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D014664:Vasodilation / Q000187:drug effects*; D014665:Vasodilator Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D001596:Benzylamines; D063065:Organophosphonates; D014665:Vasodilator Agents