为了发现针对ryanodine受体(RyRs)的有效杀虫剂,设计并合成了一系列含有N-取代苯基吡唑的新型邻氨基苯甲酰胺二酰胺类似物(12a – 12u)。这些化合物通过1 H NMR,13 C NMR和HRMS进行表征,并且化合物12u的结构通过X射线衍射确认。它们的杀虫活性表明这些化合物显示出中等至优异的活性。特别是,12i在0.25和0.05 mg L –1时对东方粘虫(Mythimna separata)表现出100%和37%的杀幼虫活性,相当于对氯吡虫啉(100%,0.25 mg L )的杀幼虫活性。–1 ; 和33%,0.05 mg L –1)。12i对小菜蛾(Plutella xylostella)的活性在0.05 mg L –1时为95%,而对照在0.05 mg L –1时为100%。钙成像技术实验结果表明,12i对神经元细胞内钙离子浓度([Ca 2+ ] i)的影响与浓度有
Tricyclic Heteroaromatic Systems. Synthesis and A1 and A2a Adenosine Binding Activities of Some 1-Aryl-1,4-dihydro-3-methyl[1]benzopyrano[2,3-c]pyrazol-4-ones, 1-Aryl-4,9-dihydro-3-methyl-1H-pyrazolo[3,4-b]quinolin-4-ones, and 1-Aryl-1H-imidazo[4,5-b]quinoxalines
The syntheses and A1 and A2aadenosinebindingactivities of some new 1-aryl-1,4-dihydro-3-methyl[1]benzopyrano[2,3-c]pyrazol-4-ones, 1-aryl-4,9-dihydro-3-methyl-1H-pyrazolo[3,4-b]-quinolin-4-ones, and 1-aryl-1H-imidazo[4,5-b]quinoxalines are reported. Some compounds show A1adenosine receptor affinity and selectivity. Structure-activity relationships on these new classes of adenosine receptor ligands