ArticleBioorganic & medicinal chemistry letters2018
Discovery of benzothiazole amides as potent antimycobacterial agents.
Article in Bioorganic & medicinal chemistry letters, 2018. 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.
- Combined computational and classical medicinal chemistry procedure to disclose novel pyrrole-based compounds as potential antituberculosis agents.Journal of computer-aided molecular design · 2026Article
- Tailored phenyl ureas eradicate drug-resistantChemical science · 2025Article
- FeBMC chemistry · 2025Article
- Antitubercular activity of 2-mercaptobenzothiazole derivatives targetingRSC medicinal chemistry · 2024Article
- Recent advances in the synthesis of new benzothiazole based anti-tubercular compounds.RSC advances · 2023Review
- Identification of 2-Amino Benzothiazoles with Bactericidal Activity against Mycobacterium tuberculosis.Microbiology spectrum · 2023Article
- Microbiological profile, preclinical pharmacokinetics and efficacy of CRS0393, a novel antimycobacterial agent targeting MmpL3.Tuberculosis (Edinburgh, Scotland) · 2023Article
- Why Matter Matters: Fast-TrackingMolecules (Basel, Switzerland) · 2022Review
- Novel chemical entities inhibiting Mycobacterium tuberculosis growth identified by phenotypic high-throughput screening.Scientific reports · 2022Article
- Mycobacterium abscessus drug discovery using machine learning.Tuberculosis (Edinburgh, Scotland) · 2022Article
- The multi-target aspect of an MmpL3 inhibitor: The BM212 series of compounds bind EthR2, a transcriptional regulator of ethionamide activation.Cell surface (Amsterdam, Netherlands) · 2021Article
- An anti-tuberculosis compound screen using a zebrafish infection model identifies an aspartyl-tRNA synthetase inhibitor.Disease models & mechanisms · 2021Article
- The Antimalarial Mefloquine Shows Activity againstInternational journal of molecular sciences · 2021Article
- Pipeline of anti-Mycobacterium abscessus small molecules: Repurposable drugs and promising novel chemical entities.Medicinal research reviews · 2021Review
- MmpL3 Inhibition: A New Approach to Treat Nontuberculous Mycobacterial Infections.International journal of molecular sciences · 2020Review
- 1Antimicrobial agents and chemotherapy · 2019Article
- Discovery of benzothiazole amides as potent antimycobacterial agents.Bioorganic & medicinal chemistry letters · 2018Article
- Optimization and Lead Selection of Benzothiazole Amide Analogs Toward a Novel Antimycobacterial Agent.Frontiers in microbiology · 2018Article
- New therapeutic strategies forExpert review of anti-infective therapyReview
Corrections and comments
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Authors and funding
11 authors.
Funding
Abstract
From a high throughput screening of commercially available libraries against nontuberculous mycobacteria and Mycobacterium tuberculosis, numerous hits were identified with moderate activity. Extensive medicinal chemistry optimization has led to a series of potent benzothiazole amide antimycobacterial agents. Replacement of the adamantyl group with cyclohexyl derivatives and further development of this series resulted in an advanced lead compound, CRS400393, which demonstrated excellent potency and a mycobacteria-specific spectrum of activity. MIC values ranged from 0.03 to 0.12 μg/mL against Mycobacterium abscessus and other rapid-grower NTM, and 1-2 μg/mL against Mycobacterium avium complex. The preliminary mechanism of action studies suggested these agents may target MmpL3, a mycobacterial mycolic acid transporter. The series has demonstrated in vivo efficacy in a proof of concept mouse model of M. abscessus infection.
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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.