Two-decades of successful SAR-grounded stories of the novel bacterial topoisomerase inhibitors (NBTIs)

Kolarič, Anja (author), Anderluh, Marko (author), Minovski, Nikola (author)

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 also provide at least interim effective protection against emerging bacterial infections. Research into DNA gyrase and topoisomerase IV inhibitors has become a particular focus, with the description of a new class of bacterial topoisomerase type II inhibitors known as "novel bacterial topoisomerase inhibitors" NBTIs. Elucidation of the key structural modifications incorporated into these inhibitors and the impact these can have on their general physicochemical properties are detailed in this review. This defines novel bacterial topoisomerase inhibitors with promising antibacterial activities and potencies, which thus represent one potential example of the future "drugs for bad bugs", as identified by the World Health Organization.

• Language: English
• Keywords: DNA gyrase inhibitors, antibacterials, novel bacterial topoisomerase inhibitors, intercalators
• Work type: Article
• Typology: 1.01 - Original Scientific Article
• Organization: FFA - Faculty of Pharmacy
• Publication status: Published
• Publication version: Version of Record
• Year: 2020
• Number of pages: Str. 5664-5674
• Numbering: Vol. 63, iss. 11
• PID: 20.500.12556/RUL-141883
• UDC: 615.015.8
• ISSN on article: 0022-2623
• DOI: 10.1021/acs.jmedchem.9b01738
• COBISS.SI-ID: 4880241
• Publication date in RUL: 10.10.2022

Record is a part of a journal

• Title: Journal of medicinal chemistry
• Shortened title: J. med. chem.
• Publisher: American Chemical Society
• ISSN: 0022-2623
• COBISS.SI-ID: 25763328

Licences

• License: CC BY 4.0, Creative Commons Attribution 4.0 International
• Link: http://creativecommons.org/licenses/by/4.0/
• Description: This is the standard Creative Commons license that gives others maximum freedom to do what they want with the work as long as they credit the author.

Secondary language

• Language: Slovenian
• Keywords: zaviralci DNA giraze, topoizomeraza tip II

Projects

• Funder: ARRS - Slovenian Research Agency
• Project number: P1-0208-2015
• Name: Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin

• Funder: ARRS - Slovenian Research Agency
• Project number: P1-0017-2015
• Name: Modeliranje kemijskih procesov in lastnosti spojin