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Synthesis and Antimicrobial Activity of 4‐Chloro‐3‐Nitrophenylthiourea Derivatives Targeting Bacterial Type II Topoisomerases
Author(s) -
Bielenica Anna,
Stępień Karolina,
Napiórkowska Agnieszka,
AugustynowiczKopeć Ewa,
Krukowski Sylwester,
Włodarczyk Marta,
Struga Marta
Publication year - 2016
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12723
Subject(s) - antimicrobial , topoisomerase , chemistry , combinatorial chemistry , microbiology and biotechnology , biology , biochemistry , organic chemistry , dna
A series of novel 4‐chloro‐3‐nitrophenylthiourea derivatives were synthesized and evaluated for their antimicrobial, antibiofilm and tuberculostatic activities. Most of compounds exhibited high antibacterial activity against both standard and hospital strains ( MIC values 0.5–2 μ g/mL), as compared to Ciprofloxacin. Derivatives with 3,4‐dichlorophenyl ( 11 ) and 3‐chloro‐4‐methylphenyl ( 13 ) substituents were the most promising towards Gram‐positive pathogens. Both of them exhibited antibiofilm potency and effectively inhibited the formation of biofilms of methicillin‐resistant and standard strains of Staphylococcus epidermidis . Two N ‐alkylthioureas ( 20, 21 ) showed twofold to fourfold increase in in vitro potency against isolates of Mycobacterium tuberculosis, as compared to Isoniazid. An action of 7, 10 , 11, 13, 20 and 21 against activity of topoisomerases isolated from Staphylococcus aureus was studied. Synthesized compounds were found as non‐genotoxic.

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