ArticleMolecules (Basel, Switzerland)2015
Design, synthesis and antitubercular activity of certain nicotinic Acid hydrazides.
Article in Molecules (Basel, Switzerland), 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed.
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- Pd-, Cu-, and Ni-Catalyzed Reactions: A Comprehensive Review of the Efficient Approaches towards the Synthesis of Antibacterial Molecules.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Synthesis, Anti-Bacterial and Molecular Docking Studies of Arylated Butyl 2-Bromoisonicotinate Against Clinical Isolates of ESBL-ProducingInfection and drug resistance · 2023Article
- Development of Novel Isatin-Tethered Quinolines as Anti-Tubercular Agents against Multi and Extensively Drug-ResistantMolecules (Basel, Switzerland) · 2022Article
- New pyrazolone derivatives, synthesis, characterization, and neuroprotective effect against PTZ- induced neuroinflammation in mice.Iranian journal of basic medical sciences · 2022Article
- A Mini Review on Isatin, an Anticancer Scaffold with Potential Activities against Neglected Tropical Diseases (NTDs).Pharmaceuticals (Basel, Switzerland) · 2022Review
- Microscale Parallel Synthesis of Acylated Aminotriazoles Enabling the Development of Factor XIIa and Thrombin Inhibitors.ChemMedChem · 2021Article
- Oxidations of Benzhydrazide and Phenylacetic Hydrazide by Hexachloroiridate(IV): Reaction Mechanism and Structure-Reactivity Relationship.Molecules (Basel, Switzerland) · 2020Article
- Synthesis and in vitro anticancer activity of certain novel 1-(2-methyl-6-arylpyridin-3-yl)-3-phenylureas as apoptosis-inducing agents.Journal of enzyme inhibition and medicinal chemistry · 2019Article
- Synthesis and biological evaluation of certain hydrazonoindolin-2-one derivatives as new potent anti-proliferative agents.Journal of enzyme inhibition and medicinal chemistry · 2018Article
- Pyridine-Ureas as Potential Anticancer Agents: Synthesis and In Vitro Biological Evaluation.Molecules (Basel, Switzerland) · 2018Article
- Novel Thiazolidinone/Thiazolo[3,2-Molecules (Basel, Switzerland) · 2018Article
- Antibacterial, Antitubercular and Antiviral Activity Evaluations of Some Arylidenehydrazide Derivatives Bearing Imidazo[2,1-Turkish journal of pharmaceutical sciences · 2017Article
- Synthesis and Herbicidal Activity of New Hydrazide and Hydrazonoyl Derivatives.Molecules (Basel, Switzerland) · 2015Article
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4 authors.
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No grant is acknowledged in the PubMed record.
Abstract
Three series of 6-aryl-2-methylnicotinohydrazides 4a-i, N'-arylidene-6-(4-bromophenyl)-2-methylnicotino hydrazides 7a-f, and N'-(un/substituted 2-oxoindolin-3-ylidene)-6-(4-fluorophenyl)-2-methylnicotinohydrazides 8a-c were synthesized and evaluated for their potential in vitro antimycobacterial activity against M. tuberculosis. The results showed that isatin hydrazides 8a-c are remarkably more active than the parent hydrazide 4c. Hydrazides 8b and 8c exhibited the highest activity among all the tested compounds (MIC = 12.5 and 6.25 µg/mL, respectively). Compounds 8b and 8c were also devoid of apparent cytotoxicity to HT-29, PC-3, A549, HepG2 and MCF-7 cancer cell lines. Besides, 8b and 8c showed good drug-likeness scores of 0.62 and 0.41, respectively. Those two isatin hydrazides could offer an excellent framework for future development to obtain more potent antitubercular agents. The SAR study suggested that lipophilicity of the synthesized derivatives is a crucial element that accounts for their antimycobacterial activity. Finally, a theoretical kinetic study was established to predict the ADME of the active derivatives.
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