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Synthesis and investigation of new indole-containing vinyl sulfide derivatives: In silico and in vitro studies for potential therapeutic applications.
Bonato Wille, Ana Paula; Pereira da Motta, Ketlyn; Pinto Brites, Nathan; Luchese, Cristiane; Frederico Schumacher, Ricardo; Antunes Wilhelm, Ethel.
Afiliación
  • Bonato Wille AP; Postgraduate Program in Biochemistry and Bioprospecting, Research Laboratory in Biochemical Pharmacology (LaFarBio), Center for Chemical, Pharmaceutical and Food Sciences, Federal University of Pelotas, Pelotas, Brazil CEP, 96010-900, RS, Brazil.
  • Pereira da Motta K; Postgraduate Program in Biochemistry and Bioprospecting, Research Laboratory in Biochemical Pharmacology (LaFarBio), Center for Chemical, Pharmaceutical and Food Sciences, Federal University of Pelotas, Pelotas, Brazil CEP, 96010-900, RS, Brazil.
  • Pinto Brites N; Department of Chemistry, Federal University of Santa Maria, Santa Maria Brazil, CEP, 97105-900, RS, Brazil.
  • Luchese C; Postgraduate Program in Biochemistry and Bioprospecting, Research Laboratory in Biochemical Pharmacology (LaFarBio), Center for Chemical, Pharmaceutical and Food Sciences, Federal University of Pelotas, Pelotas, Brazil CEP, 96010-900, RS, Brazil.
  • Frederico Schumacher R; Department of Chemistry, Federal University of Santa Maria, Santa Maria Brazil, CEP, 97105-900, RS, Brazil.
  • Antunes Wilhelm E; Postgraduate Program in Biochemistry and Bioprospecting, Research Laboratory in Biochemical Pharmacology (LaFarBio), Center for Chemical, Pharmaceutical and Food Sciences, Federal University of Pelotas, Pelotas, Brazil CEP, 96010-900, RS, Brazil.
Chem Biodivers ; 21(2): e202301460, 2024 Feb.
Article en En | MEDLINE | ID: mdl-38117615
ABSTRACT
Indoles featuring organosulfur compounds serve as privileged structural scaffolds in various biologically active compounds. This study investigates the biological properties of five synthetic sulphenyl vinyl indoles (3 a-e) using both in silico and in vitro methods. Computational analyses employing Swiss ADME and Molinspiration software reveal the remarkable inhibitory activity of compound 3 d against proteases and kinases (scores of 0.18 and 0.06, respectively). Furthermore, it demonstrates the ability to modulate ionic and G protein-coupled receptors (scores -0.06 and 0.31, respectively) and serves as a ligand for nuclear receptors (score 0.15). In vitro investigations highlight the compounds' efficacy in countering ABTS+ radical attacks and reducing lipid peroxidation levels. Particularly noteworthy is the superior efficacy of compounds 3 a, 3 b, and 3 e in DPPH (EC50 3 a 268.5 µM) and TEAC assays (EC50 3 a 49.9 µM; EC50 3 b 133.4 µM, and EC50 3 e 84.9 µM), as well as TBARS levels. Compound 3 c significantly reduces acetylcholinesterase activity, positioning itself as a noteworthy enzyme inhibitor. This study emphasizes the versatile biological potential of synthetic indole derivatives, suggesting their applicability for therapeutic purposes.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Acetilcolinesterasa / Sulfuros / Antioxidantes Idioma: En Revista: Chem Biodivers Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2024 Tipo del documento: Article País de afiliación: Brasil Pais de publicación: Suiza
Texto completo
Añadir a Mi BVS
Imprimir
XML
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Acetilcolinesterasa / Sulfuros / Antioxidantes Idioma: En Revista: Chem Biodivers Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2024 Tipo del documento: Article País de afiliación: Brasil Pais de publicación: Suiza