Influence of partially hydrogenated pyridines (derivatives of cyanothioacetamide) on blood indicators of rats with acute tetrachloromethane hepatitis

Anna A. Burdeynaya, E. Bibik, B. S. Krivokolysko, K. Frolov, V. Dotsenko, S. Krivokolysko
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Abstract

: Currently, a focused search for new and safe hepatoprotective agents is highly relevant. An experimental study was conducted on 80 male rats after intragastric infiltration of carbon tetrachloride (CCl 4 ) in a 50% solution of refined sunflower oil intragastrically once a day at a dose of 4 ml/kg for 3 days. Screening researches of six partially hydrogenated pyridines, derivatives of cyanothioacetamide, on a model of acute tetracycline hepatitis at a dose of 5 mg/kg showed a high hepatoprotective and detoxifying activity in all compounds. They stabilize the level of biochemical blood parameters, keeping them at the normal level in terms of hepatotoxicity induced by the use of high dosages of CCl 4 in vivo. A compound CV146 (benzyl 4- (4-chlorophenyl) -5-cyano-6 - ({2 - [(3,4-dimethylphenyl) amino] -2-oxoethyl} thio) -2-methyl-1,4-dihydropyridine -3-carboxylate) should be considered as an perspective in terms of further preclinical studies in order to find new highly effective and safe agents for the pharmacocorrection of acute toxic liver damages. cyanothioacetamide, tetrachloromethane hepatitis model. named after St. Luke. liver damage was in once a day at dose 4 ml/kg For research, we used substituted di- tetrahydropyridines with the codes CV042, CV043, CV046, CV047, CV080, CV146 compound CV146 with those in intact animals, a decrease of 25.6% is seen. The activity of transaminases in the blood of rats of this experimental group was reduced by 25.5% (ALT) and 39.2% (AST) compared with the control group. Alkaline phosphatase activity was at the level recorded in the group of intact animals. these properties be considered as an further find new highly effective
部分氢化吡啶(氰硫乙酰胺衍生物)对急性四氯甲烷肝炎大鼠血液指标的影响
目前,重点寻找新的和安全的肝保护药物是高度相关的。实验研究了80只雄性大鼠在50%的精制葵花籽油溶液中灌胃四氯化碳(ccl4),每天1次,剂量为4 ml/kg,连续3天。对6种部分氢化吡啶类氰硫乙酰胺衍生物在急性四环素型肝炎模型上5 mg/kg剂量的筛选研究表明,所有化合物均具有较高的保肝和解毒活性。它们稳定了血液生化参数的水平,使它们在体内高剂量ccl4引起的肝毒性方面保持在正常水平。化合物CV146(苄基4-(4-氯苯基)-5-氰基-6 -({2 -[(3,4-二甲基苯基)氨基]-2-氧乙基}硫)-2-甲基-1,4-二氢吡啶-3-羧酸盐)应作为进一步临床前研究的前景,以寻找新的高效安全的药物来纠正急性中毒性肝损伤。氰硫乙酰胺、四氯甲烷肝炎模型。以圣路加命名。研究中,我们使用编码为CV042、CV043、CV046、CV047、CV080、CV146的替代二-四氢吡啶,与正常动物的CV146相比,降低了25.6%。与对照组相比,实验组大鼠血液中转氨酶活性分别降低25.5% (ALT)和39.2% (AST)。碱性磷酸酶活性维持在正常对照组的水平。这些特性被认为是进一步发现新的高效
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