Synthesis and bioactivity of substituted alpha-aminobenzylphosphonate.
- Author:
Li-zhi ZHAO
1
;
Ri-fang YANG
;
Ru-sheng ZHAO
;
Yan-fang ZHANG
;
Dong-mei CHEN
;
Hai WANG
Author Information
- Publication Type:Journal Article
- MeSH: Animals; Aorta; drug effects; Benzylamines; chemical synthesis; chemistry; pharmacology; Guinea Pigs; Ileum; drug effects; Molecular Structure; Muscle Contraction; drug effects; Organophosphonates; chemical synthesis; chemistry; pharmacology; Rats; Vasodilation; drug effects; Vasodilator Agents; chemical synthesis; chemistry; pharmacology
- From: Acta Pharmaceutica Sinica 2006;41(4):342-345
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo search for some substituted alpha-amino phosphonates as leading compounds with the vasodilator effects.
METHODSTarget 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.
RESULTSSeven 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.
CONCLUSIONTwo (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.
