Rajasekaran Aiyalu, Murugesan Sankaranarayanan, AnandaRajagopal Kalasalingam
Asian Institute of Medicine, Science and Technology, Kedah Darul Aman, Malaysia.
Arch Pharm Res. 2006 Jul;29(7):535-40. doi: 10.1007/BF02969261.
Several novel 1-[2-(1H-tetrazol-5-yl) ethyl]-1H-benzo[d][1,2,3]triazoles (3a-h) have been synthesized by the condensation of 1-[2-(1H-tetrazol-5-yl)-ethyl]-1H-benzotriazole (2) and appropriate acid chlorides. 1-[2-(1H-tetrazol-5-yl)-ethyl]-1H-benzotriazole (2) was synthesized by reacting 3-(1H-benzo[d][1,2,3]triazol-1-yl)propanenitrile with sodium azide and ammonium chloride in the presence of dimethylformamide. The synthesized compounds were characterized by IR and PMR analysis. The titled compounds were evaluated for their in-vitro antibacterial and antifungal activity by the cup plate method and anticonvulsant activity evaluated by the maximal electroshock induced convulsion method in mice. All synthesized compounds exhibited moderate antibacterial activity against Bacillus subtilis and moderate antifungal activity against Candida albicans. Compounds 5-(2-(1H-benzo[d][1,2,3]triazo-1-yl)ethyl)-1H-tetrazol-1-yl)(4-aminophenyl)methanone 3d and 5-(2-(1 H-benzo[d][1,2,3]triazo-1-yl)ethyl)-1H-tetrazol-1-yl)(2-aminophenyl)methanone 3e elicited excellent anticonvulsant activity.
通过1-[2-(1H-四唑-5-基)乙基]-1H-苯并三唑(2)与适当的酰氯缩合，合成了几种新型的1-[2-(1H-四唑-5-基)乙基]-1H-苯并[d][1,2,3]三唑(3a-h)。1-[2-(1H-四唑-5-基)乙基]-1H-苯并三唑(2)是通过使3-(1H-苯并[d][1,2,3]三唑-1-基)丙腈与叠氮化钠和氯化铵在二甲基甲酰胺存在下反应合成的。通过红外光谱和核磁共振分析对合成的化合物进行了表征。通过杯碟法评估了标题化合物的体外抗菌和抗真菌活性，并通过最大电休克诱导惊厥法在小鼠中评估了其抗惊厥活性。所有合成的化合物对枯草芽孢杆菌均表现出中等抗菌活性，对白色念珠菌表现出中等抗真菌活性。化合物5-(2-(1H-苯并[d][1,2,3]三唑-1-基)乙基)-1H-四唑-1-基)(4-氨基苯基)甲酮3d和5-(2-(1H-苯并[d][1,2,3]三唑-1-基)乙基)-1H-四唑-1-基)(2-氨基苯基)甲酮3e表现出优异的抗惊厥活性。
