ArticleJournal of medicinal chemistry2013
SAR studies on trisubstituted benzimidazoles as inhibitors of Mtb FtsZ for the development of novel antitubercular agents.
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed.
- Experimental and theoretical studies on antituberculosis activity of different benzimidazole derivatives.Heliyon · 2025Article
- A Review of Approaches to the Metallic and Non-Metallic Synthesis of Benzimidazole (BnZ) and Their Derivatives for Biological Efficacy.Molecules (Basel, Switzerland) · 2023Review
- Investigating the Antituberculosis Activity of Selected Commercial Essential Oils and Identification of Active Constituents Using a Biochemometrics Approach and In Silico Modeling.Antibiotics (Basel, Switzerland) · 2022Article
- Synthetic approaches to potent heterocyclic inhibitors of tuberculosis: A decade review.Frontiers in pharmacology · 2022Review
- Structure-activity relationship studies on 2,5,6-trisubstituted benzimidazoles targetingRSC medicinal chemistry · 2021Article
- Tuberculosis Drug Discovery: A Decade of Hit Assessment for Defined Targets.Frontiers in cellular and infection microbiology · 2021Review
- Synthesis and Antimycobacterial Activity of 2,5-Disubstituted and 1,2,5-Trisubstituted Benzimidazoles.Frontiers in chemistry · 2020Article
- 3D QSAR-based design and liquid phase combinatorial synthesis of 1,2-disubstituted benzimidazole-5-carboxylic acid and 3-substituted-5MedChemComm · 2019Article
- Novel T9 loop conformation of filamenting temperature-sensitive mutant Z from Mycobacterium tuberculosis.Acta crystallographica. Section F, Structural biology communications · 2019Article
- New Application of Neomycin B-Bisbenzimidazole Hybrids as Antifungal Agents.ACS infectious diseases · 2018Article
- Strategic incorporation of fluorine in the drug discovery of new-generation antitubercular agents targeting bacterial cell division protein FtsZ.Journal of fluorine chemistry · 2017Article
- Design and Synthesis of Some Novel Fluorobenzimidazoles Substituted with Structural Motifs Present in Physiologically Active Natural Products for Antitubercular Activity.Iranian journal of pharmaceutical research : IJPR · 2017Article
- Recent advances in the discovery and development of antibacterial agents targeting the cell-division protein FtsZ.Bioorganic & medicinal chemistry · 2016Review
- Synthesis and investigation of novel benzimidazole derivatives as antifungal agents.Bioorganic & medicinal chemistry · 2016Article
- Targeting the Bacterial Division Protein FtsZ.Journal of medicinal chemistry · 2016Review
- Cell division inhibitors with efficacy equivalent to isoniazid in the acute murine Mycobacterium tuberculosis infection model.The Journal of antimicrobial chemotherapy · 2015Article
- Drug discovery targeting cell division proteins, microtubules and FtsZ.Bioorganic & medicinal chemistry · 2014Review
- Design, synthesis and evaluation of novel 2,5,6-trisubstituted benzimidazoles targeting FtsZ as antitubercular agents.Bioorganic & medicinal chemistry · 2014Article
- A trisubstituted benzimidazole cell division inhibitor with efficacy against Mycobacterium tuberculosis.PloS one · 2014Article
Corrections and comments
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Authors and funding
5 authors.
Funding
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.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.