Study of Toxic Effects of Oxothiazole Derivative as a New Antibacterial Agent

Q4 Veterinary
H. Beyzaei, A. Jamshidian, M. Hajinezhad, S. Hashemi, Nasim Amel, Maliheh Abdollahi, Fatemeh Arab-Sahebi, Behzad Ghasemi
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引用次数: 0

Abstract

The spread of antibiotic-resistant bacteria in many humans and animals has driven researches to identify and design novel antibacterial agents. In vitro inhibitory activity of (2E)-2-(4,5-dihydro-4-oxothiazol-2-yl)-2-(thiazolidin-2-ylidene) acetonitrile against many bacterial pathogens has been proven in both veterinary and human medicine. In this study, its in vivo toxic effects was studied in mice. The median lethal dose (LD50) value of 239.88 mg/kg was estimated using intraperitoneal injection in 8 groups of mice after 48 h treatment. Then, intraperitoneal injections of LD50 of oxothiazole solution into 4 other mice were done to evaluate histopathological changes in their liver and kidney tissues. The histopathological studies were identified as fatty change, hepatitis, necrosis and regeneration in liver, and fibrosis, necrosis, nephritis, hyaline cast and hyperaemia in kidney. In conclusion, the synthesized oxothiazole derivative causes renal and hepatic toxicity in mice at medium concentrations. The change of thiazole substituents and complexation may reduce its toxicity.
新型抗菌剂Oxothiazole衍生物的毒性研究
抗生素耐药细菌在许多人类和动物中的传播推动了研究鉴定和设计新的抗菌剂。(2E)-2-(4,5-二氢-4-氧噻唑-2-基)-2-(噻唑烷-2-酰基)乙腈对多种细菌病原体的体外抑制作用已在兽药和人药中得到证实。本研究对其在小鼠体内的毒性作用进行了研究。8组小鼠经48 h腹腔注射,估计中位致死剂量(LD50)为239.88 mg/kg。然后,对另外4只小鼠腹腔注射LD50的氧噻唑溶液,观察其肝脏和肾脏组织的病理变化。组织病理学检查确定为肝脏脂肪改变、肝炎、坏死和再生,肾脏纤维化、坏死、肾炎、透明样变和充血。综上所述,所合成的氧噻唑衍生物在中等浓度下对小鼠具有肾和肝毒性。噻唑取代基和络合的变化可降低其毒性。
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CiteScore
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