Synthesis and evaluation for anticonvulsant activity of some N-(5-(substituted)-1,3,4-thiadiazol-2-yl)-2-((5-(substituted)-4H-1,2,4-triazol-3-yl)-amino) acetamide derivatives

D. Rishipathak, Luketa Alai, P. Udavant
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Abstract

Several new promising bioactive derivatives of N-(5-(Substituted)-1, 3, 4-thiadiazol-2-yl)-2-((5-(substitutes)-4H-1, 2, 4-triazol-3-yl) amino) acetamide were synthesized. The compounds were obtained in excellent yields. The synthesized compounds were confirmed on the basis of IR and NMR. Acute toxicity study was done to determine the LD50 of the newly synthesized compounds. Some of the synthesized compounds were evaluated for their anticonvulsant effect by PTZ induced convulsions method. Statistical testing was done by one way ANOVA followed by Dunnett’s test. The compounds D-III showed the highest percentage of protection as compared to PTZ, i.e. 80% at the dose of 20mg/kg among the evaluated compounds compared to control. Keywords: 1, 3, 4-thiadiazole, 1, 2, 4-triazole, Anticonvulsant
若干N-(5-(取代)-1,3,4-噻二唑-2-基)-2-((5-(取代)- 4h -1,2,4-三唑-3-基)氨基)乙酰胺衍生物的合成及抗惊厥活性评价
合成了N-(5-(取代)- 1,3,4 -噻二唑-2-基)-2-((5-(取代)- 4h - 1,2,4 -三唑-3-基)氨基)乙酰胺的几种具有生物活性的新衍生物。这些化合物的收率很高。合成的化合物经红外光谱和核磁共振确证。对新合成的化合物进行了急性毒性研究,测定了LD50。用PTZ诱发惊厥法评价了部分合成化合物的抗惊厥作用。统计检验采用单因素方差分析和邓尼特检验。与PTZ相比,化合物D-III显示出最高的保护百分比,在20mg/kg剂量下,与对照相比,评价化合物中D-III的保护百分比为80%。关键词:1,3,4 -噻二唑,1,2,4 -三唑,抗惊厥药
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