Anti-inflammatory, analgesic and COX-2 inhibitory activity of novel thiadiazoles in irradiated rats

Ragab, F. M.; Heiba, Helmy I.; El‐Gazzar, Marwa G.; Abou‐Seri, Sahar M.; El-Sabbagh, Walaa A.; El‐Hazek, Reham M. M.

doi:10.1016/j.jphotobiol.2016.12.007

Cited by 42 publications

(13 citation statements)

References 48 publications

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“…According to Kere sk enyiov a & Smajda (2004) findings, that effect could be attributed to the release of endogenous opioids after radiation exposure. Similar findings were reported by other authors (El-Ghazaly et al, 2017;Ragab et al, 2017).…”

Section: Discussionsupporting

confidence: 93%

Effect of nanostructured lipid carriers on transdermal delivery of tenoxicam in irradiated rats

et al. 2020

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Transdermal delivery of non-steroidal anti-inflammatory drugs (NSAIDs) is an effective route of drug administration, as it directs the drug to the inflamed site with reduced incidence of systemic adverse effects such as gastric hemorrhage and ulcers. Tenoxicam (TNX) is a member of NSAIDs that are marketed only as oral tablets due to very poor absorption through the skin. The current study intended to formulate and characterize a hydrogel loaded with nanostructured lipid carriers (NLCs) to enhance the transdermal delivery of TNX. Six formulations of TNX were formulated by slight modifications of high shear homogenization and ultrasonication method. The selected formula was characterized for their particle size, polydispersity index (PDI), zeta potential, entrapment efficiency (EE), in-vitro drug release and ex-vivo skin permeation studies. Moreover, the effectiveness of the developed formula was studied in-vivo using carrageenan-induced paw edema and hyperalgesia model in irradiated rats. Formula F4 was chosen from six formulations, as the average diameter was 679.4 ± 51.3 nm, PDI value of about 0.02, zeta potential of À4.24 mV, EE of 92.36%, globules nanoparticles without aggregations and absence of interactions in the developed formula. Additionally, the in-vivo study showed the efficacy of formula F4 (TNX-NLCs hydrogel) equivalent to oral TNX in reducing the exaggerated inflammatory response induced by carrageenan after irradiation. In conclusion, the present findings suggest that TNX-NLCs hydrogel could be a potential transdermal drug delivery system alternative to the oral formulation for the treatment of various inflammatory conditions.

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Section: Discussionsupporting

confidence: 93%

Effect of nanostructured lipid carriers on transdermal delivery of tenoxicam in irradiated rats

et al. 2020

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“…From the pharmacological point of view, the analysed 1,3,4-tiadiazoles [ 5 , 6 ] substituted with the resorcylic fragment have been observed to have promising anticancer [ 7 , 8 , 9 , 10 ] and neuroprotective [ 11 , 12 , 13 ], anti-oxidative [ 7 ], antifungal and antibacterial activities [ 14 , 15 , 16 , 17 ], anti-inflammatory [ 18 ]. They also show certain very interesting properties as a group of ligands capable of forming complexes with selected D-block metals [ 6 ].…”

Section: Introductionmentioning

confidence: 99%

Spectroscopic Studies of Dual Fluorescence in 2-(4-Fluorophenylamino)-5-(2,4-dihydroxybenzeno)-1,3,4-thiadiazole: Effect of Molecular Aggregation in a Micellar System

et al. 2018

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The article presents the results of spectroscopic studies focused on a selected compound from the 1,3,4-thiadiazole group—2-(4-fluorophenylamino)-5-(2,4-dihydroxybenzeno)-1,3,4-thia-diazole (FABT)—in a micellar system formed by Triton X-100, a non-ionic detergent. Fluorescence measurements revealed the phenomenon of dual fluorescence whose emergence is related to the particular molecular organisation of the compound, which depends both on the concentration of the detergent and, most of all, the concentration of the compound itself. Dual fluorescence of FABT in a micellar system was observed for the compound dissolved in a methanol aqueous system, i.e., an environment wherein the dual fluorescence of the compound had never been reported before. Based on the interpretation of UV-Vis electronic absorption, resonance light scattering (RLS), emission and excitation fluorescence spectra, as well as measurements of dynamic light scattering (DLS) and Principal Component Analysis (PCA), we were able to relate the occurrence of this effect to the process of molecular aggregation taking place between FABT molecules in the micellar system in question. Results of fluorescence spectra measurements and time-correlated single photon counting (TCSPC) indicate that dual fluorescence occurs at detergent concentrations necessary to form micellar systems, which in turn facilitate the process of aggregation of FABT molecules. The correlation between the observed fluorescence effects and the previous measurements performed for analogues from this group suggests the possibility of charge transfer (CT) within the range of detergent concentrations wherein the aforementioned fluorescence effects are observed. It ought to be emphasised that this type of fluorescence effects are relatively easy to induce, which predisposes this groups of fluorophores as ideal fluorescence probes in the context of biological samples.

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“…Among these molecules, thiadiazoles, which have an important place among the 5-membered heterocyclic containing nitrogen and sulfur, are widely used in pharmaceutical chemistry, materials science and organic synthesis (Shahcheragh et al, 2017). 1,3,4-Thiadiazole and its derivatives have a broad spectrum of biological activity such as antimicrobial (El-Gohary et al, 2013), antibacterial (Li et al, 2015), antioxidant (Gür et al, 2017), anticonvulsant (Luszczki et al, 2015), analgesic (Ragab et al, 2016), and anticancer (Polkam et al, 2017). In addition, 1,3,4-thiadiazole derivatives are widely used in bactericides, insecticides, pesticides, fungicides and herbicides in many areas of agriculture and technology (Zarei, 2017;Zou et al, 2002).…”

Section: Introductionmentioning

confidence: 99%

Yeni 5-Merkapto-2-(5-metil-furan-2-il-metilidenamino)-1,3,4-tiyadiazol Molekülün Sentezi ve Teorik Analizi

Kotan

Medetalibetoğlu

Beytur

et al. 2019

Iğdır Üniversitesi Fen Bilimleri Enstitüsü Dergisi

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In this study, the novel 5-Mercapto-2-(5-methyl-furan-2-yl-methylidenamino)-1,3,4thiadiazole molecule was synthesized from the reaction of 2-amino-5-mercapto-1,3,4-thiadiazole with 5-methyl-furan-2-carbaldehyde. The 5-Mercapto-2-(5-methyl-furan-2-yl-methylidenamino)-1,3,4thiadiazole was optimized by using DFT(B3LYP)-HF methods. The mulliken charges, HOMO-LUMO energy, E LUMO-E HOMO energy gap (ΔEg), dipole moments, electron affinity (A), ionization potential (I), chemical softness (σ), chemical hardness (η), electronegativity (χ), bond angles, total energy and bond lengths of the molecule were calculated by using 6-31G(d,p) basis set with DFT (B3LYP) and HF methods. Otherwise, the 1 H-NMR and 13 C-NMR isotropic shift values were calculated by using GIAO methods with GaussianG09W package program. The experimental/theoretical values were compared and the regression analysis were found. Defining IR values were used the veda4f program. The theoretical infrared spectrums are visualised.

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Anti-inflammatory, analgesic and COX-2 inhibitory activity of novel thiadiazoles in irradiated rats

Cited by 42 publications

References 48 publications

Effect of nanostructured lipid carriers on transdermal delivery of tenoxicam in irradiated rats

Effect of nanostructured lipid carriers on transdermal delivery of tenoxicam in irradiated rats

Spectroscopic Studies of Dual Fluorescence in 2-(4-Fluorophenylamino)-5-(2,4-dihydroxybenzeno)-1,3,4-thiadiazole: Effect of Molecular Aggregation in a Micellar System

Yeni 5-Merkapto-2-(5-metil-furan-2-il-metilidenamino)-1,3,4-tiyadiazol Molekülün Sentezi ve Teorik Analizi

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