Abstract
BackgroundIn recent years, 1, 2, 4-triazole and its derivatives have been reported to be pharmacologically significant scaffolds. They possess analgesic, anti-tubercular, anti-inflammatory, anti-convulsant, anti-oxidant, anti-fungal, anti-cancer, anxiolytic and anti-depressant activity. This study was designed and conducted to evaluate the potential anti-inflammatory, analgesic and antipyretic activities of Triazole derivatives.MethodsSwiss albino (male and female) mice weighing 20-30 g (10-24 weeks female), (5-14 weeks male) and Wister Kyoto rats (male and female) weighing 200-300 g (8-10 weeks old) were used for the present study. Anti-inflammatory activity was checked using Lambda carrageenan (λ) and egg albumin-induced paw edema models. Analgesic via Writhing Reflex induced by acetic acid and formalin, furthermore anti-pyretic activity was assessed by yeast induced pyrexia.ResultsBoth of the test compounds exhibited encouraging anti-inflammatory analgesic and antipyretic results when compared with standard drug ibuprofen. The maximum inhibition of edema for the compound (S)-1-(4-Amino-5-mercapto-4H-1,2,4-triazole-3-yl) ethanol [3] was found to be (91)% as compared to reference drug ibuprofen (82)%, while (S)-1-(6-Phenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazin-3-yl)ethanol [5e] showed equipotent results to ibuprofen (81)%. The derivatives were also screened for their anti-nociceptive activity by Acetic acid writhing and tail immersion test. Compound 3 showed a significant reduction in wriths (83)% as compared to standard drug ibuprofen 71.5% and [5] showed comparable results to ibuprofen by exhibiting 70% reduction in writh at the same dose as that of standard drug, moreover, there were no signs of toxicity being observed after administration of high doses of test compounds to mice.ConclusionsIt is evident from the results that compounds 3(compound A) and 5(compound B) are a potential candidate for anti-inflammatory, analgesic and anti-pyretic and the scaffold could be used for further structural modifications. Further studies would help to evaluate their molecular mechanism of action regarding these beneficial activities.
Highlights
In recent years, 1, 2, 4-triazole and its derivatives have been reported to be pharmacologically significant scaffolds
It is evident from the results that compounds 3(compound A) and 5(compound B) are a potential candidate for anti-inflammatory, analgesic and anti-pyretic and the scaffold could be used for further structural modifications
Apart from analgesic and anti-inflammatory studies, the anti-pyretic activity of 1, 2, 4 triazole derivatives have been assessed by the yeast method in rats, declared that all the synthesized compounds inherent antipyretic activity [31]. All these studies provide us with encouraging evidence of significant anti-pyretic, analgesic and anti-inflammatory effects of 1,2,4 Triazole and enhance their importance as future candidates in multiple disease treatments. We extended this ongoing research by conducting and reporting, in-vivo evaluation of antiinflammatory, analgesic and antipyretic activities of newly synthesized derivatives of 1,2,4-triazole, namely compound A, (S)-1-(4-Amino-5-mercapto- 4H-1,2,4
Summary
1, 2, 4-triazole and its derivatives have been reported to be pharmacologically significant scaffolds. They possess analgesic, anti-tubercular, anti-inflammatory, anti-convulsant, anti-oxidant, anti-fungal, anti-cancer, anxiolytic and anti-depressant activity. This study was designed and conducted to evaluate the potential anti-inflammatory, analgesic and antipyretic activities of Triazole derivatives. Inflammations have been reported to operate during severe perturbations of homeostasis, such as tissue injury, infections, exposure to contaminants. Pain is an unpleasant experience evoked by tissue injury or potential, noxious (i.e., tissue-damaging) stimuli. Transmission and perception are very extensive and complex interplays between signalling systems, modulation from higher centres, involving fundamental biological events at various levels of the nervous system and the unique perception of the individual [4]
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