Background In 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. Methods Swiss 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. Results Both 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. Conclusions 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. Further studies would help to evaluate their molecular mechanism of action regarding these beneficial activities.

The research work focuses on investigating the effects of spacer group (varying aliphatic chain length=n) of co-crystal formers (oxalic acid (OA, n=0), (malonic acid (MA, n=1), (succinic acid (SA, n=2), (glutaric acid (GA, n=3), and (adipic acid (AA, n=4) on the physicochemical properties and oral bioavailability of praziquantel (PZQ) co-crystals. For this purpose, different co-crystals of PZQ with dicarboxylic acid co-crystal formers (OA, MA, SA, GA, and AA) were synthesized. These co-crystals were characterized by powder X-ray diffractometry (XRPD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), and thermogravimetry (TG) techniques. The in-vitro (solubility and dissolution) and in-vivo pharmacokinetic (P.K) studies were performed for PZQ co-crystals. Additionally, the effect of polymer hydroxypropyl cellulose (HPC) on the formation of PZQ co-crystals was also investigated. According to the study results, PZQ-SA co-crystal showed improved solubility, dissolution, and oral bioavailability. Overall, the solubility, dissolution, and oral bioavailability are consistent with each other. The order of improved solubility, dissolution, and oral bioavailability is observed as consistent like PZQ-SA > PZQ-AA > PZQ-GA > PZQ-OA > PZQ-MA > pure PZQ. Concerning HPC polymer effects, PZQ-OA, PZQ-MA, PZQ-GA, and PZQ-AA co-crystals were formed successfully in the presence of HPC polymer but the PZQ-SA co-crystal was inhibited.

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