Abstract

Background and Aim: The 1H-perimidne, as novel source carbene ligand, is well known for its anti-fungal, anti-microbial or anti-tumor activities. Here, we aimed to study the acute toxicity in Wistar rat of 2-(2,3-dihydro-1H-perimidin-2-yl)-6-methoxyphenol, a new heterocyclic 1H- perimidine synthetized in our laboratory. 
 Materials and Methods: Five groups of males Wistar rats were intraperitoneally injected with 7 mg/kg, 40 mg/kg, 90 mg/kg, 130 mg/kg and 150 mg/kg dissolved in dimethyl sulfoxide (DMSO), and followed during 14 days. We noted any clinical signs of acute toxicity as body weight loss, salivation, tremor, convulsion among others, as well as food consumption and water intake level.
 Results: The DL50 of the new 2-(2,3-dihydro-1H-perimidin-2-yl)-6-methoxyphenol was estimated to 65 mg/kg. The No Observed Adverse Effect Level (NOAEL) dose was 7 mg/kg because it did not caused mortality, clinical signs of acute toxicity, and not affected feed and water intake behavior. However, significant abnormalities as inflammation and necrosis were observed at doses-effects dependent in liver, when compared to NOAEL dose and vehicle.
 Conclusion: The new heterocyclic 2-(2,3-dihydro-1H-perimidin-2-yl)-6-methoxyphenol is considered as high toxicity grade product. From NOAEL dose, subsequent biological, toxicological, pharmacological and neurobehavioral studies are needed before using for clinical trials.

Highlights

  • The synthesis of new chemicals is worthwhile to be tested for the environmental or health safety

  • We study here the acute toxicity with a single intraperitoneal injection of 2-(2,3-dihydro

  • The acute toxicity test was carried out according the guideline of Organization for Economic Cooperation and Development (i.e OECD)

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Summary

Introduction

The synthesis of new chemicals is worthwhile to be tested for the environmental or health safety. The 1H-perimidine system is well known as a major source of novel carbene ligand [2]. A past work focused on the synthesis a florescent heterocycle of 1H-perimidine compound 4-(2,3dihydro-1H-périmidin-2yl)-2-methoxyphenol) with out testing either lethal dose or biological activities [6]. The 1H-perimidne, as novel source carbene ligand, is well known for its anti-fungal, anti-microbial or anti-tumor activities. We aimed to study the acute toxicity in Wistar rat of 2-(2,3-dihydro-1H-perimidin-2-yl)-6-methoxyphenol, a new heterocyclic 1H- perimidine synthetized in our laboratory. The No Observed Adverse Effect Level (NOAEL) dose was 7 mg/kg because it did not caused mortality, clinical signs of acute toxicity, and not affected feed and water intake behavior. From NOAEL dose, subsequent biological, toxicological, pharmacological and neurobehavioral studies are needed before using for clinical trials

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