Antimicrobial and cytotoxic activities of 1,2,3-triazole-sucrose derivatives.

Autor: Petrova KT; LAQV, REQUIMTE, Departamento de Química, Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa, 2829-516 Caparica, Portugal. Electronic address: k.petrova@fct.unl.pt., Potewar TM; LAQV, REQUIMTE, Departamento de Química, Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa, 2829-516 Caparica, Portugal., Correia-da-Silva P; Instituto Superior de Ciências da Saúde Egas Moniz, 2829-511 Caparica, Portugal., Barros MT; LAQV, REQUIMTE, Departamento de Química, Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa, 2829-516 Caparica, Portugal., Calhelha RC; Mountain Research Centre (CIMO), ESA, Polytechnic Institute of Bragança, Campus de Santa Apolónia, 1172, 5301-855 Bragança, Portugal., Ćiric A; Department of Plant Physiology, Institute for Biological Research, 'Siniša Stanković', University of Belgrade, Bulevar Despota Stefana 142, 11000 Belgrade, Serbia., Soković M; Department of Plant Physiology, Institute for Biological Research, 'Siniša Stanković', University of Belgrade, Bulevar Despota Stefana 142, 11000 Belgrade, Serbia., Ferreira IC; Mountain Research Centre (CIMO), ESA, Polytechnic Institute of Bragança, Campus de Santa Apolónia, 1172, 5301-855 Bragança, Portugal.
Jazyk: angličtina
Zdroj: Carbohydrate research [Carbohydr Res] 2015 Nov 19; Vol. 417, pp. 66-71. Date of Electronic Publication: 2015 Sep 15.
DOI: 10.1016/j.carres.2015.09.003
Abstrakt: A library of 1-(1',2,3,3',4,4',6-hepta-O-acetyl-6'-deoxy-sucros-6'-yl)-1,2,3-triazoles have been investigated for their antibacterial, antifungal and cytotoxic activities. Most of the target compounds showed good inhibitory activity against a variety of clinically and food contaminant important microbial pathogens. In particular, 1-(1',2,3,3',4,4',6-hepta-O-acetyl-6'-deoxy-sucros-6'-yl)-4-(4-pentylphenyl)-1,2,3-triazole (5) was highly active against all the tested bacteria with minimal inhibitory concentrations (MICs) ranging between 1.1 and 4.4 µM and bactericidal concentrations (MBCs) from 2.2 and 8.4 µM. The compound 1-(1',2,3,3',4,4',6-hepta-O-acetyl-6'-deoxy-sucros-6'-yl)-4-(4-bromophenyl)-1,2,3-triazole (3) showed antifungal activity with MICs from 0.6 to 4.8 µM and minimal fungicidal concentrations (MFCs) ranging between 1.2 and 8.9 µM. Furthermore, some of the compounds possessed moderate cytotoxicity against human breast, lung, cervical and hepatocellular carcinoma cell lines, without showing toxicity for non-tumor liver cells. The above mentioned derivatives represent promising leads for the development of new generation of sugar-triazole antifungal agents.
(Copyright © 2015 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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