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• W2069793608 abstract "FtsZ, an essential protein for bacterial cell division, is a highly promising therapeutic target, especially for the discovery and development of new-generation anti-TB agents. Following up the identification of two lead 2,5,6-trisubstituted benzimidazoles, 1 and 2, targeting Mtb-FtsZ in our previous study, an extensive SAR study for optimization of these lead compounds was performed through systematic modification of the 5 and 6 positions. This study has successfully led to the discovery of a highly potent advanced lead 5f (MIC = 0.06 μg/mL) and several other compounds with comparable potencies. These advanced lead compounds possess a dimethylamino group at the 6 position. The functional groups at the 5 position exhibit substantial effects on the antibacterial activity as well. In vitro experiments such as the FtsZ polymerization inhibitory assay and TEM analysis of Mtb-FtsZ treated with 5f and others indicate that Mtb-FtsZ is the molecular target for their antibacterial activity." @default.
• W2069793608 created "2016-06-24" @default.
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• W2069793608 date "2013-11-23" @default.
• W2069793608 modified "2023-09-23" @default.
• W2069793608 title "SAR Studies on Trisubstituted Benzimidazoles as Inhibitors of <i>Mtb</i> FtsZ for the Development of Novel Antitubercular Agents" @default.
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• W2069793608 doi "https://doi.org/10.1021/jm401468w" @default.
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