ArticleThe Journal of antibiotics2019
Benzaldehyde thiosemicarbazone derivatives against replicating and nonreplicating Mycobacterium tuberculosis.
Article in The Journal of antibiotics, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed.
- New thiosemicarbazones: synthesis, structural characterization, in vitro, and in silico evaluation of antiproliferative effects.Future medicinal chemistry · 2025Article
- Plant-Derived Compounds in Hemp Seeds (Molecules (Basel, Switzerland) · 2024Review
- Exploration of morpholine-thiophene hybrid thiosemicarbazones for the treatment of ureolytic bacterial infections via targeting urease enzyme: Synthesis, biochemical screening and computational analysis.Frontiers in chemistry · 2024Article
- Synthesis and Structure-Activity Relationship of 2,6-Disubstituted Thiosemicarbazone Derivatives of Pyridine as Potential Antituberculosis Agents.Materials (Basel, Switzerland) · 2023Article
- QSAR Studies, Molecular Docking, Molecular Dynamics, Synthesis, and Biological Evaluation of Novel Quinolinone-Based Thiosemicarbazones againstAntibiotics (Basel, Switzerland) · 2022Article
- X-ray Structures and Computational Studies of Two Bioactive 2-(Adamantane-1-carbonyl)-Molecules (Basel, Switzerland) · 2022Article
- Acetylene containing 2-(2-hydrazinyl)thiazole derivatives: design, synthesis, andRSC advances · 2022Article
- Structure-Based Virtual Screening of Benzaldehyde Thiosemicarbazone Derivatives against DNA Gyrase B ofEvidence-based complementary and alternative medicine : eCAM · 2021Article
- Characterization and Release Behavior of a Thiosemicarbazone from Electrospun Polyvinyl Alcohol Core-Shell Nanofibers.Polymers · 2020Article
- Novel isoniazid derivative as promising antituberculosis agent.Future microbiology · 2020Article
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
In this article, we report a series of benzaldehyde thiosemicarbazone derivatives possessing high activity toward actively replicating Mycobacterium tuberculosis strain with minimum inhibitory concentration (MIC) values in the range from 0.14 to 2.2 μM. Among them, two compounds-2-(4-phenethoxybenzylidene)hydrazine-1-carbothioamide (13) and 2-(3-isopropoxybenzylidene)hydrazine-1-carbothioamide (20) also demonstrate submicromolar antimycobacterial activity against M. tuberculosis under hypoxia with MIC values of 0.68 and 0.74 μM, respectively. The activity of compounds 13 and 20 toward five investigated isoniazid-, rifampicin-, and fluoroquinolone-resistant M. tuberculosis isolates is similar to commercially available antituberculosis drugs. The compounds 13 and 20 possess good ADME properties and have low cytotoxicity toward human liver cells (HepG2). Therefore, 2-(4-phenethoxybenzylidene)hydrazine-1-carbothioamide (13) and 2-(3-isopropoxybenzylidene)hydrazine-1-carbothioamide (20) are valuable candidates for further preclinical studies.
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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.