Novel Bacterial Topoisomerase inhibitors (NBTIs) – A comprehensive review
Autor: | Jigar Desai, Sanjay Kumar, Rajiv Sharma, S. Sachchidanand |
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Rok vydání: | 2021 |
Předmět: |
Topoisomerase
biology NBTI Topoisomerase IV medicine.drug_class Chemistry DNA gyrase biology.organism_classification Small molecule RS1-441 Other systems of medicine Pharmacy and materia medica Antibiotic resistance Mechanism of action Biochemistry medicine biology.protein hERG MIC medicine.symptom RZ201-999 Bacteria Topoisomerase inhibitor |
Zdroj: | European Journal of Medicinal Chemistry Reports, Vol 3, Iss, Pp 100017-(2021) |
ISSN: | 2772-4174 |
DOI: | 10.1016/j.ejmcr.2021.100017 |
Popis: | Bacterial DNA gyrase and topoisomerase IV inhibition has emerged as a promising strategy for the cure of infections caused by antibiotic-resistant bacteria. Small molecule antibacterials inhibiting bacterial topoisomerases have been previously exploited by the successful fluoroquinolone class. The Novel Bacterial Topoisomerase Inhibitors (NBTIs) bind to a different site to that of the fluoroquinolones with novel mechanism of action to evade the existing target-mediated bacterial resistance associated with fluoroquinolones. This review comprehensively summarizes various efforts with respect to structural modifications of inhibitors and their impact on their general physicochemical and biological properties. |
Databáze: | OpenAIRE |
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