Abstract
The quinoxaline derivatives are an important class of heterocyclic compounds, obtained from chemical azote replacement of carbone atom. Fusion of quinoxaline production is relatively easy as they are obviously synthesized by the fusion of two aromatic rings, benzene and pyrazine. The new quinoxalinique derivative, 6-nitro-2 (1H)-quinoxalinone (NQX), has been synthesized in our laboratory. However, the related toxic effect on rat remains unknown. The present work aims to study the acute toxicity of NQX in normal Wistar rats. Seven groups of female rats received an intraperitoneal (i.p.) injection of 0 (control), 20, 40, 60, 120, 200 and 300 mg/kg of the NQX and followed for 14 days. Mortalities, behavioural changes, weight, changes in food and water uptake, urine output and weight of faeces were monitored. At the end of the experiment, the rats receiving the no-observed-adverse-effect level (NOAEL) are sacrificed, blood and organs were collected and haematological and biochemical parameters were analysed in sera sample. The results showed that the NQX Lethal Dose 50 (LD50) was 161.16 mg/kg. The administration of NQX at a dose of 40 mg/kg (NOAEL dose) did not affect animal viability and body weight. In addition, food intake, water intake and urine output remain unchanged. Furthermore, at the NOAEL dose, the levels of blood cells (erythrocytes and leukocytes), haemoglobin, biochemical parameters (glucose, cholesterol, triglycerides, urea, creatinine, bilirubin, total protein and transaminase) and organ’s weights (liver, kidney, spleen, pancreas, heart and brain) were not affected. NQX seems to be relatively saved at the dose of 40 mg/kg in normal Wistar rats and could possibly be tested after further analysis in a preliminary clinical test.
Highlights
Quinoxaline or benzopyrazine is a heterocyclic compound containing a benzene and pyrazine ring
Our results showed that the lethal minimum dose (LMD) of the nitro-2 (1H)-quinoxalinone (NQX) tested is 60 mg/kg, whereas the LD is 120 mg/kg and 200 mg/kg (Table 1, Figure 4)
The Lethal Dose 50 (LD50) of the NQX is estimated at 161.16 mg/kg
Summary
Quinoxaline or benzopyrazine is a heterocyclic compound containing a benzene and pyrazine ring. Pyrazines are colourless compounds, which are stable and possess good water solubility. Unlike pyridines, they are expensive, hardly available and are rarely used as the starting material for the synthesis of their derivatives. Diazines are bonded to the benzene ring to create quinoxaline. The quinoxaline derivatives are an important class of heterocyclic compounds, in which N replaces one or more carbon atoms of the naphthalene ring (Deepika et al, 2011). The main location to the quinoxaline loop system is shown, whereas 2 and 3 are placed at alpha-positions (Chesseman & Cookson, 1979) The main location to the quinoxaline loop system is shown in Figure 1, whereas 2 and 3 are placed at alpha-positions (Chesseman & Cookson, 1979)
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