We have investigated the antibacterial activity of some new steroidal thiosemicarbazones and their Pd(II) metal complexes were prepared by the reaction of the thiosemicarbazones with [Pd(DMSO)2Cl2].
Abdullah M. Asiri, Salman A. Khan
doaj +2 more sources
Antifungal activities of thiosemicarbazones and semicarbazones against mycotoxigenic fungi
Mycotoxigenic fungi can compromise the quality of food, exposing human and animal health at risk. The antifungal activity of eight thiosemicarbazones (1-8) and nine semicarbazones (9-17) was evaluated against Aspergillus flavus, A. nomius, A.
Rojane de Oliveira Paiva +4 more
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Structural Studies of 2,6-Diacetyl- and 2,6-Diformylpyridine Bis(thiosemicarbazones)
Although a large number of crystal structures of heterocyclic thiosemicarbazones have recently appeared in the literature, few structures of heterocyclic bis(thiosemicarbazones) or their metal complexes have been reported.
Brown Christine A. +4 more
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Pyridyl-Thiazole-Thiosemicarbazones as Antitrypanosomatidae Agents: Design, Synthesis, and In Silico Profiling. [PDF]
A novel pyridine–thiazole derivative, Compound 8, exhibited potent dual antitrypanosomatid activity. It demonstrated remarkable in vitro efficacy against Trypanosoma cruzi (IC50 = 1.0 µM) and L. amazonensis (IC50 = 3.9 µM). Molecular docking studies suggested interactions with heme and multiple molecular targets.
Silva AJFSD +10 more
europepmc +2 more sources
Evolution of Thiosemicarbazones: From First- to Second-Generation Metal Chelators and Their Reactive Oxygen Species-Mediated Effects in Melanoma. [PDF]
Thiosemicarbazones (TSC) have demonstrated promise as new chemotherapeutic agents against melanoma in both in vitro and In vivo studies. TSC are powerful metal coordinating agents, coordinating transition metal ions such as zinc, copper and iron in multiple oxidation states. It is this metal coordination that imparts the anticancer activity.
Alim R, Andrew SD, Parkinson CJ.
europepmc +2 more sources
Cruzain Inhibitors for Chagas Disease: Anticorrelated Optimisation Landscapes and the Multiparametric Path to Clinical Candidates. [PDF]
Three decades of cruzain‐targeted drug discovery have yielded 215 sub‐micromolar inhibitors but no clinical candidates. This review diagnoses a systemic translational failure driven by single‐parameter optimisation and proposes a multiparametric framework integrating enzymatic potency, cathepsin selectivity, intracellular exposure, and metabolic ...
Dos Reis CRC +7 more
europepmc +2 more sources
Monoamine Oxidase and Cholinesterase Inhibition Profiles of Semicarbazone and Thiosemicarbazone Derivatives. [PDF]
Thiosemicarbazones generally show higher MAO‐B inhibitory potential than their corresponding semicarbazones, and particularly T6 is the most potent, which contains R = H and X = S in its Tail Unit, with an IC50 value of 6.45 µM with SI of 3.6. ABSTRACT Twenty semicarbazone and thiosemicarbazone derivatives (T1–T20) were synthesized and evaluated for ...
Bindra S +11 more
europepmc +2 more sources
A Thiosemicarbazone Schiff Base and Its Titanium(IV) Complexes: Spectral Analysis, DFT Studies, and Biological Evaluation. [PDF]
DFT computations are used to analyze the electronic structure, stability, and reactivity profiles of a new Schiff base ligand and its Ti(IV) complexes and are characterized by elemental analysis, IR, 1H NMR, 13C NMR, and mass spectrometry and screened for antimicrobial activities against E. coli, S. aureus, ESBL, MRSA, Mtb, A.
Ghanghas P +6 more
europepmc +2 more sources
Multidrug resistance (MDR) mediated by P-glycoprotein (Pgp) represents a significant impediment to successful cancer treatment. The compound, di-2-pyridylketone 4,4-dimethyl-3-thiosemicarbazone (Dp44mT), has been shown to induce greater cytotoxicity ...
Duraippandi Palanimuthu +11 more
core +3 more sources
A set of 12 monosubstituted acetophenone thiosemicarbazone derivatives (TSCs) were synthesized and their inhibitory properties toward tyrosinase activity were tested.
Katarzyna Hałdys +4 more
doaj +1 more source

