ArticleACS medicinal chemistry letters2019
Spirocyclic and Bicyclic 8-Nitrobenzothiazinones for Tuberculosis with Improved Physicochemical and Pharmacokinetic Properties.
Article in ACS medicinal chemistry letters, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
14 citing papers in PubMed, 44 citations in OpenAlex.
- Exploring the Natural Products Atlas (NPAtlas) Database for Hunting Prospective Irreversible Covalent DprE1 Inhibitors With Antitubercular Activity: An IntegratedJournal of tropical medicine · 2026Article
- Challenges of Aufheben to Promote Druglikeness: Chemical Modification Strategies to Improve Aqueous Solubility and Permeability.Journal of medicinal chemistry · 2025Review
- Overcoming colorectal cancer and cancer stem cell resistance with photodynamic therapy: new frontiers in oncology.RSC advances · 2025Review
- Side Chain-Modified Benzothiazinone Derivatives with Anti-Mycobacterial Activity.Biomedicines · 2023Article
- Recent Advances of DprE1 Inhibitors againstACS omega · 2022Review
- BTZ-Derived Benzisothiazolinones with In Vitro Activity againstACS medicinal chemistry letters · 2022Article
- Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistantRSC medicinal chemistry · 2022Article
- Development of 6-Methanesulfonyl-8-nitrobenzothiazinone Based Antitubercular Agents.ACS medicinal chemistry letters · 2022Article
- New Insight into Dearomatization and Decarbonylation of Antitubercular 4H-Benzo[e][1,3]thiazinones: Stable 5H- and 7H-Benzo[e][1,3]thiazines.ChemMedChem · 2022Article
- Efficient Synthesis of Benzothiazinone Analogues with Activity against Intracellular Mycobacterium tuberculosis.ChemMedChem · 2022Article
- 2-Chloro-3-nitro-5-(tri-fluoro-meth-yl)benzoic acid and -benzamide: structural characterization of two precursors for anti-tubercular benzo-thia-zinones.Acta crystallographica. Section E, Crystallographic communications · 2021Article
- 8-cyanobenzothiazinone analogs with potent antitubercular activity.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2021Article
- Crystallographic evidence for unintended benzisothiazolinone 1-oxide formation from benzothiazinones through oxidation.Acta crystallographica. Section C, Structural chemistry · 2020Article
- Antibiotics in the clinical pipeline in October 2019.The Journal of antibiotics · 2020Review
Corrections and comments
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Authors and funding
3 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
8-Nitrobenzothiazinones (BTZs) typified by the second-generation analogue PBTZ169 are a new class of antitubercular agents. The activity of BTZs and lipophilicity are tightly coupled since the molecular target DprE1 is located in the mycobacterial cell envelope. A series of analogues was designed to address the notorious insolubility of the BTZs while preserving the required lipophilicity. This was accomplished by decreasing the molecular planarity and symmetry through bioisosteric replacement of the piperazine moiety of PBTZ169 with spirocyclic and bicyclic diamines. Several promising compounds with improved aqueous solubilities were identified with potent antitubercular activity. Compound
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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.