Category: Triazoles. Shaikh, M; Siddiqui, S; Zafar, H; Naqeeb, U; Subzwari, F; Imad, R; Khan, KM; Choudhary, MI in [Shaikh, Muniza; Zafar, Humaira; Subzwari, Fakiha; Imad, Rehan; Choudhary, Muhammad I.] Univ Karachi, Dr Panjwani Ctr Mol Med & Drug Res, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan; [Siddiqui, Salman; Naqeeb, Uzma; Khan, Khalid M.; Choudhary, Muhammad I.] Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan; [Khan, Khalid M.] Imam Abdulrahman Bin Faisal Univ, Inst Res & Med Consultat IRMC, Dept Clin Pharm, POB 31441, Dammam, Saudi Arabia; [Choudhary, Muhammad I.] King Abdulaziz Univ, Dept Biochem, Fac Sci, Jeddah 21412, Saudi Arabia published Antiglycation Activity of Triazole Schiff’s Bases Against Fructose-mediated Glycation: In Vitro and In Silico Study in 2020.0, Cited 59.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5.
Background: Advanced glycation end products (AGEs) are known to be involved in the pathophysiology of diabetic complications, neurodegenerative diseases, and aging. Preventing the formation of AGEs can be helpful in the management of these diseases. Objectives: Two classes of previously synthesized traizole Schiff’s bases (4H-1,2,4-triamle-4-Schiff’s bases 1-14, and 4H-1,2,4-triazole-3-Schiff’s bases 15-23) were evaluated for their in vitro antiglycation activity. Methods: In vitro fructose-mediated human serum albumin (HSA) glycation assay was employed to assess the antiglycation activity of triazole Schiff’s bases. The active compounds were subjected to cytotoxicity analysis by MTT assay on mouse fibroblast (3T3) cell line. Molecular docking and simulation studies were carried out to evaluate the interactions and stability of compounds with HSA. Anti-hyperglycemic and antioxidant activities of selected non-cytotoxic compounds were evaluated by in vitro a-glucosidase inhibition, and DPPH free radical scavenging assays, respectively. Results: Compound 1 (IC50 =47.30 +/- 0.38 mu M) from 4H-1,2,4-triazole-4-Schiff’s bases has exhibited antiglycation activity comparable to standard rutin (IC50 =54.5 +/- 0.05 mu M) along with a stable RMSD profile in MD simulation studies. Compound 1 also exhibited a potent a-glucosidase inhibitory activity, and moderate antioxidant property. Other derivatives showed a weak antiglycation activity with IC50 values between 248.1-637.7 mu M. Compounds with potential antiglycation profile were found to be non-cytotoxic in a cellular assay. Conclusion: The study identifies triazole Schiff s bases active against fructose-mediated glycation of HSA, thus indicates their potential against late diabetic complications due to production of advancedend products (AGEs).
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Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
1,2,3-Triazole – Wikipedia,
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