Second-generation 4,5,6,7-tetrahydrobenzo[d]thiazoles as novel DNA gyrase inhibitors
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چکیده
منابع مشابه
Cyclothialidine analogs, novel DNA gyrase inhibitors.
DNA gyrase inhibitors, cyclothialidines B, C, D and E were isolated from four Streptomycete strains (NR 0659, NR 0660, NR 0661 and NR 0662). Their structures have been elucidated based on the amino acid analysis of the hydrolysates, NMR and HRFAB-MS experiments and shown to be cyclothialidine analogs. The absolute stereochemistry has been determined by the chiral HPLC analysis of the hydrolysat...
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Methods: Structure of DNA gyrase (2XCT) was retrieved from the Protein Data Bank (PDB) and the structures of (FQ) compounds were selected from literature survey of 400 novel compounds and the physical, chemical and molecular characteristics of each compound were obeyed for drugrelevant properties based on “Lipinski’s rule of five, then a total of 150 (FQ)s were docked against the protein of the...
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Bacterial DNA gyrase is a well-established and validated target for the development of novel antibacterials. Starting from the available structural information about the binding of the natural product inhibitor, clorobiocin, we identified a novel series of 4'-methyl-N(2)-phenyl-[4,5'-bithiazole]-2,2'-diamine inhibitors of gyrase B with a low micromolar inhibitory activity by implementing a two-...
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cells are known to require ATP for all catalytic activities. However, during the purification of the enzymes, some of their native properties may be lost due to proteolytic degradation or to a resolution of their supramolecular structure (Glikin et al., 1984). The trypanosomal extracts, as well as the enzyme obtained after hydroxylapatite chromatography, are capable of catenating supercoiled ci...
متن کاملidentification of novel bacterial dna gyrase inhibitors: an in silico study
owing to essential role in bacterial survival, dna gyrase has been exploited as a validated drug target. however, rapidly emerging resistance to gyrase-targeted drugs such as widely utilized fluoroquinolones reveals the necessity to develop novel compounds with new mechanism of actions against this enzyme. here, an attempt has been made to identify new drug-like molecules for shigella flexneri ...
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ژورنال
عنوان ژورنال: Future Medicinal Chemistry
سال: 2020
ISSN: 1756-8919,1756-8927
DOI: 10.4155/fmc-2019-0127