ArticleACS medicinal chemistry letters2014
2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.
Article in ACS medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed.
- Design, Synthesis, Antimycobacterial Evaluation, and In Silico Investigation of Benzisothiazole-Based Hydrazide Derivatives as Potential Anti-Tuberculosis Agents.Chemical biology & drug design · 2026Article
- New pyrazole-based derivatives targeting MmpL3 transporter in Mycobacterium tuberculosis: design, synthesis, biological evaluation and molecular docking studies.Molecular diversity · 2025Article
- Exploration of pyrazole-based pyridine-4-carbohydrazide derivatives as drug-resistantFuture medicinal chemistry · 2025Article
- An arylsulfonamide that targets cell wall biosynthesis inAntimicrobial agents and chemotherapy · 2024Article
- Synthetic approaches to potent heterocyclic inhibitors of tuberculosis: A decade review.Frontiers in pharmacology · 2022Review
- Access to Bicyclo[4.2.0]octene Monomers To Explore the Scope of Alternating Ring-Opening Metathesis Polymerization.The Journal of organic chemistry · 2018Article
- Syntheses and evaluation of multicaulin and miltirone-like compounds as antituberculosis agents.Journal of enzyme inhibition and medicinal chemistry · 2017Article
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Authors and funding
19 authors.
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Abstract
A cellular activity-based screen on Mycobacterium tuberculosis (Mtb) H37Rv using a focused library from the AstraZeneca corporate collection led to the identification of 2-phenylindoles and arylsulphonamides, novel antimycobacterial scaffolds. Both the series were bactericidal in vitro and in an intracellular macrophage infection model, active against drug sensitive and drug resistant Mtb clinical isolates, and specific to mycobacteria. The scaffolds showed promising structure-activity relationships; compounds with submicromolar cellular potency were identified during the hit to lead exploration. Furthermore, compounds from both scaffolds were tested for inhibition of known target enzymes or pathways of antimycobacterial drugs including InhA, RNA polymerase, DprE1, topoisomerases, protein synthesis, and oxidative-phosphorylation. Compounds did not inhibit any of the targets suggesting the potential of a possible novel mode of action(s). Hence, both scaffolds provide the opportunity to be developed further as leads and tool compounds to uncover novel mechanisms for tuberculosis drug discovery.
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