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Anticholinesterase activity of ß-carboline-1, 3, 5-triazine hybrids
Baréa, Paula; Barbosa, Valéria Aquilino; Yamazaki, Diego Alberto dos Santos; Gomes, Carla Maria Beraldi; Novello, Claudio R; Costa, Willian Ferreira da; Gauze, Gisele de Freitas; Sarragiotto, Maria Helena.
  • Baréa, Paula; State University of Maringá. Chemistry Department. BR
  • Barbosa, Valéria Aquilino; State University of Maringá. Chemistry Department. BR
  • Yamazaki, Diego Alberto dos Santos; State University of Maringá. Chemistry Department. BR
  • Gomes, Carla Maria Beraldi; State University of Maringá. Chemistry Department. BR
  • Novello, Claudio R; Federal Technological University of Paraná. Department of Chemistry and Biology. Francisco Beltrão. BR
  • Costa, Willian Ferreira da; State University of Maringá. Chemistry Department. BR
  • Gauze, Gisele de Freitas; State University of Maringá. Chemistry Department. BR
  • Sarragiotto, Maria Helena; State University of Maringá. Chemistry Department. BR
Braz. J. Pharm. Sci. (Online) ; 58: e19958, 2022. tab, graf
Article in English | LILACS | ID: biblio-1383955
ABSTRACT
Abstract The ß-carboline-1,3,5-triazine hydrochlorides 8-13 were evaluated in vitro against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The analysed compounds were selective to BuChE, with IC50 values in the range from 1.0-18.8 µM being obtained. The N-{2-[(4,6-dihydrazinyl-1,3,5-triazin-2-yl)amino]ethyl}-1-phenyl-ß-carboline-3-carboxamide (12) was the most potent compound and kinetic studies indicate that it acts as a competitive inhibitor of BuChE. Molecular docking studies show that 12 strongly interacts with the residues of His438 (residue of the catalytic triad) and Trp82 (residue of catalytic anionic site), confirming that this compound competes with the same binding site of the butyrylthiocholine
Subject(s)


Full text: Available Index: LILACS (Americas) Main subject: Triazines / In Vitro Techniques Language: English Journal: Braz. J. Pharm. Sci. (Online) Journal subject: Farmacologia / Terapˆutica / Toxicologia Year: 2022 Type: Article Affiliation country: Brazil Institution/Affiliation country: Federal Technological University of Paraná/BR / State University of Maringá/BR

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Full text: Available Index: LILACS (Americas) Main subject: Triazines / In Vitro Techniques Language: English Journal: Braz. J. Pharm. Sci. (Online) Journal subject: Farmacologia / Terapˆutica / Toxicologia Year: 2022 Type: Article Affiliation country: Brazil Institution/Affiliation country: Federal Technological University of Paraná/BR / State University of Maringá/BR