An article Novel [1,2,3] triazolo[1,5-a]pyridine derivatives are trypanocidal by sterol biosynthesis pathway alteration WOS:000478848800005 published article about CELL-PROLIFERATION; STRUCTURAL-BASIS; DRUG CANDIDATES; CHOLESTEROL; 14-ALPHA-DEMETHYLASE; INHIBITION; INSIGHTS; BINDING; CYP51; CHAIN in [Lapier, Michel; Guzman-Rivera, Daniela; Gonzalez-Herrera, Fabiola; Pesce, Barbara; Maya, Juan D.] Univ Chile, Fac Med, Inst Ciencias Biomed ICBM, Clin & Mol Pharmacol Program, Independencia 1027, Santiago 1027, Chile; [Ballesteros-Garrido, Rafael; Ballesteros, Rafael; Abarca, Belen] Univ Valencia, Fac Pharm, Dept Organ Chem, Avda Vicent Andres Estelles S-N, E-46100 Valencia, Spain; [Aguilera-Venegas, Benjamin; Moncada-Basualto, Mauricio; Olea-Azar, Claudio] Univ Chile, Fac Chem & Pharmaceut Sci, Free Rad & Antioxidants Lab, Inorgan & Analyt Dept, Santos Dumt 964, Santiago, Chile; [Moncada-Basualto, Mauricio] Univ Santiago Chile, Fac Chem & Biol, Dept Environm Sci, Santiago, Chile; [Kemmerling, Ulrike] Univ Chile, Fac Med, Inst Ciencias Biomed ICBM, Anat & Dev Biol Program, Independencia 1027, Santiago, Chile in 2019, Cited 38. The Name is Ethyl nicotinate. Through research, I have a further understanding and discovery of 614-18-6. Recommanded Product: Ethyl nicotinate
Aim: To study a new series of [1,2,3] triazolo[1,5-alpha] pyridine derivatives as trypanocidal agents because current antichagasic pharmacologic therapy is only partially effective. Materials & methods: The effect of the series upon Trypanosoma cruzi epimastigotes and murine macrophages viability, cell cycle, cell death and on the metabolites of the sterol biosynthesis pathway was measured; also, docking in 14 alpha-demethylase was analyzed. Results: Compound 16 inhibits 14 alpha-demethylase producing an imbalance in the cholesterol/ergosterol synthesis pathway, as suggested by a metabolic control and theoretical docking analysis. Consequently, it prevented cell proliferation, stopping the cellular cycle at the G2/M phase, inducing cell death. Conclusion: Although the exact cell death mechanism remained elusive, this series can be used for the further rational design of novel antiparasitic molecules.
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Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem