ArticleAngewandte Chemie (International ed. in English)2018
Small Molecules Targeting Mycobacterium tuberculosis Type II NADH Dehydrogenase Exhibit Antimycobacterial Activity.
Article in Angewandte Chemie (International ed. in English), 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
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Who cites it
31 citing papers in PubMed, 60 citations in OpenAlex.
- From Planktonic to Sedentary Lifestyle: Molecular Dissection of the Establishment and Maintenance of Mycobacterial Biofilm.ACS omega · 2026Article
- Dual inhibition of respiratory complexes inMicrobiology spectrum · 2026Article
- Combination strategies targeting multiple ETC subunits as a rational approach for drug-resistant TB therapy.Archives of microbiology · 2026Review
- Inhibitors of NADH-O-methylquinone compound a class of antitubercular drugs.Molecular diversity · 2025Article
- Hidden Markov Model-Based Prokaryotic Genome Space Mining Reveals the Widespread Pervasiveness of Complex I and Its Potential Evolutionary Scheme.Genome biology and evolution · 2025Article
- 4(3International journal of molecular sciences · 2025Review
- Structure-based Virtual Screening and Hit Identification of Novel designed Quinazolin-4(3H)-one Derivatives as Antitubercular Agent against TargetsCurrent drug discovery technologies · 2025Article
- Antitubercular activity of 2-mercaptobenzothiazole derivatives targetingRSC medicinal chemistry · 2024Article
- CytochromeRSC medicinal chemistry · 2024Review
- Comprehensive essentiality analysis of themBio · 2023Article
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- New Insights into the Modification of the Non-Core Metabolic Pathway of Steroids inInternational journal of molecular sciences · 2023Review
- Tricyclic SpiroLactams Kill Mycobacteria In Vitro and In Vivo by Inhibiting Type II NADH Dehydrogenases.Journal of medicinal chemistry · 2022Article
- Targeting the cytochrome bcMolecular diversity · 2022Review
- Fragment-Based Drug Discovery against Mycobacteria: The Success and Challenges.International journal of molecular sciences · 2022Review
- Article
- The Orphan Response Regulator Rv3143 Modulates the Activity of the NADH Dehydrogenase Complex (Nuo) inFrontiers in cellular and infection microbiology · 2022Article
- Uncovering interactions between mycobacterial respiratory complexes to target drug-resistantFrontiers in cellular and infection microbiology · 2022Review
- Article
- Review
Corrections and comments
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Authors and funding
15 authors at 5 institutions in 2 countries.
Funding
Abstract
The generation of ATP through oxidative phosphorylation is an essential metabolic function for Mycobaterium tuberculosis (Mtb), regardless of the growth environment. The type II NADH dehydrogenase (Ndh-2) is the conduit for electrons into the pathway, and is absent in the mammalian genome, thus making it a potential drug target. Herein, we report the identification of two types of small molecules as selective inhibitors for Ndh-2 through a multicomponent high-throughput screen. Both compounds block ATP synthesis, lead to effects consistent with loss of NADH turnover, and importantly, exert bactericidal activity against Mtb. Extensive medicinal chemistry optimization afforded the best analogue with an MIC of 90 nm against Mtb. Moreover, the two scaffolds have differential inhibitory activities against the two homologous Ndh-2 enzymes in Mtb, which will allow precise control over Ndh-2 function in Mtb to facilitate the assessment of this anti-TB drug target.
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Registered trials
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.