Two Decades of Successful SAR-Grounded Stories of the Novel Bacterial Topoisomerase Inhibitors (NBTIs)
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.9b01738
Abstract: The emergence of bacterial resistance against life-saving medicines has forced the scientific community and pharmaceutical industry to take actions in the quest for novel antibacterials. These should not only overcome the existing bacterial resistance but… read more here.
Keywords: novel bacterial; topoisomerase inhibitors; topoisomerase; inhibitors nbtis ... See more keywords
1,3-Dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Expanding Structural Diversity and the Antibacterial Spectrum.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00111
Abstract: Antibacterial resistance continues its devastation of available therapies. Novel bacterial topoisomerase inhibitors (NBTIs) offer one solution to this critical issue. Two series of amine NBTIs bearing tricyclic DNA-binding moieties as well as amide NBTIs with… read more here.
Keywords: bacterial topoisomerase; novel bacterial; dioxane linked; topoisomerase inhibitors ... See more keywords
Discovery of novel bacterial topoisomerase I inhibitors by use of in silico docking and in vitro assays
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DOI: 10.1038/s41598-018-19944-4
Abstract: Topoisomerases are important targets for antibacterial and anticancer therapies. Bacterial topoisomerase I remains to be exploited for antibiotics that can be used in the clinic. Inhibitors of bacterial topoisomerase I may provide leads for novel… read more here.
Keywords: topoisomerase inhibitors; vitro assays; topoisomerase; silico screening ... See more keywords
Small DNA circles as bacterial topoisomerase I inhibitors
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DOI: 10.1039/c9ra02398d
Abstract: It is demonstrated that small DNA circles showed high inhibitory effect on the activity of bacterial topoisomerase I and the single-stranded regions associated with bending deformation are believed to be the crucial factor for trapping… read more here.
Keywords: circles bacterial; small dna; bacterial topoisomerase; dna circles ... See more keywords
Novel Bacterial Topoisomerase Inhibitors with Potent Broad-Spectrum Activity against Drug-Resistant Bacteria
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DOI: 10.1128/aac.02100-16
Abstract: ABSTRACT The novel bacterial topoisomerase inhibitor class is an investigational type of antibacterial inhibitor of DNA gyrase and topoisomerase IV that does not have cross-resistance with the quinolones. Here, we report the evaluation of the… read more here.
Keywords: novel bacterial; dna; topoisomerase; resistance ... See more keywords