[Synthesis and vascular relaxing activity of arecoline derivatives coupled with nitric oxide donors].
OBJECTIVE
To search for potential anti-atherosclerosis drugs with vascular relaxation activity, a series of agonists of endothelial targets were designed and synthesized.


METHODS
Coupling N-methyl-1,2, 3,6-tetrahydrapyridine ring system with 3,4-dibenzenesulfonyl-1,2,5-oxadiazole-2-oxide through esterification or amidation, a series of arecoline derivatives containing NO donors were designed and synthesised.


RESULTS
A novel series of compounds structurally related to arecoline have been prepared, the proposed structures of eighteen new compounds were established by IR, 1H NMR, MS spectroscopy and elemental analysis. The effects of the target compounds on the vasodilation activity were tested in the isolated preparation of mice thoratic aorta.


CONCLUSIONS
This preliminary pharmacological tests showed that the candidates have good vasodilation activities and were worthy to be intensively studied.
Huang
Sheng-Tang
ST
School of Pharmacy, Xianning College, Xianning 437100, China.
Huang
Wen-Long
WL
Zhang
Hui-Bin
HB