title: [Synthesis and bioactivity of substituted alpha-aminobenzylphosphonate].
abstract: 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.
authors.affiliation: Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing, China.
authors.forename: Li-zhi
authors.initials: LZ
authors.lastname: Zhao
authors.forename: Ri-fang
authors.initials: RF
authors.lastname: Yang
authors.forename: Ru-sheng
authors.initials: RS
authors.lastname: Zhao
authors.forename: Yan-fang
authors.initials: YF
authors.lastname: Zhang
authors.forename: Dong-mei
authors.initials: DM
authors.lastname: Chen
authors.forename: Hai
authors.initials: H
authors.lastname: Wang
mesh_terms: 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
chemical_list: D001596:Benzylamines; D063065:Organophosphonates; D014665:Vasodilator Agents