Synthesis and vascular relaxing activity of arecoline derivatives coupled with nitric oxide donors / 药学学报

<p><b>AIM</b>To search for potential anti-atherosclerosis drugs with vascular relaxation activity, a series of agonists of endothelial targets were designed and synthesized.</p><p><b>METHODS</b>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.</p><p><b>RESULTS</b>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.</p><p><b>CONCLUSION</b>This preliminary pharmacological tests showed that the candidates have good vasodilation activities and were worthy to be intensively studied.</p>

Synthesis and antibacterial activity of 3-(5-substituted phenyl-1,3,4 oxadiazole-2-yl-methylenethio)-5-pyridin-3-yl-1,2,4 triazole-4-yl-amines / 药学学报

<p><b>AIM</b>To study on synthesis and antibacterial activity evaluation of polyheterocycles.</p><p><b>METHODS</b>The condensation of 4-amino-3-pyridin-3-yl-4H-[1,2,4] triazole-5-thiol with 2-chloromethyl-5-substituted phenyl-[1,3,4] oxadiazoles gave the corresponding title heterocycle amines, and the in vitro antibacterial activity was primarily evaluated by the method of cup-plate diffusion solution.</p><p><b>RESULTS</b>Twelve novel compounds were synthesized, and their structures were confirmed by IR, 1H NMR, MS and element analysis. Biological screening results demonstrated that most of the compounds prepared showed good antibacterial activity.</p><p><b>CONCLUSION</b>Oxadiazoles incorporting pyridyl triazole ring may be a pharmacophor structure in the molecule for developing antibacterial candidate drugs.</p>

Synthesis and antibacterial activity of 2-(3-pyridyl)-5-((5-aryl-1,3,4-oxadiazol-2-yl) methylenethio)-1,3,4-oxadiazoles / 药学学报

<p><b>AIM</b>Studies on synthesis and antibacterial activity of new heterocycles.</p><p><b>METHODS</b>The cyclocondensation of [(3-pyridyl)-1,3,4-oxadiazol-2-yl] thio acetic acid with various aroyl hydrazines in the presence of POCl3 and xylene gave the corresponding titled compounds, and the in vitro antibacterial activity was primarily evaluated by the method of cupplate diffusion solution.</p><p><b>RESULTS</b>Sixteen novel titled compounds were synthesized, their structures were confirmed by IR, 1HNMR, MS and elemental analysis. Biological screening results demonstrated that most of the compounds prepared displayed potential antibacterial activity.</p><p><b>CONCLUSION</b>Oxadiazoles incorporting pyridyl oxadiazole ring may be usefully antibacterial candidate drugs.</p>