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Novel trisubstituted benzimidazoles, targeting Mtb FtsZ, as a new class of antitubercular agents.

Abstract：

:Libraries of novel trisubstituted benzimidazoles were created through rational drug design. A good number of these benzimidazoles exhibited promising MIC values in the range of 0.5-6 μg/mL (2-15 μM) for their antibacterial activity against Mtb H37Rv strain. Moreover, five of the lead compounds also exhibited excellent activity against clinical Mtb strains with different drug-resistance profiles. All lead compounds did not show appreciable cytotoxicity (IC(50) > 200 μM) against Vero cells, which inhibited Mtb FtsZ assembly in a dose dependent manner. The two lead compounds unexpectedly showed enhancement of the GTPase activity of Mtb FtsZ. The result strongly suggests that the increased GTPase activity destabilizes FtsZ assembly, leading to efficient inhibition of FtsZ polymerization and filament formation. The TEM and SEM analyses of Mtb FtsZ and Mtb cells, respectively, treated with a lead compound strongly suggest that lead benzimidazoles have a novel mechanism of action on the inhibition of Mtb FtsZ assembly and Z-ring formation.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Kumar K,Awasthi D,Lee SY,Zanardi I,Ruzsicska B,Knudson S,Tonge PJ,Slayden RA,Ojima I

doi

10.1021/jm1012006

subject

Has Abstract

pub_date

2011-01-13 00:00:00

pages

374-81

issue

1

eissn

0022-2623

issn

1520-4804

journal_volume

54

pub_type

杂志文章

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