Xn:Harmful;5351-91-7Relevant articles and documents
Synthesis, physicochemical properties, and in vitro antibacterial screening of palladium(II) complexes derived from thiosemicarbazone
Azam, Mohammad,Warad, Ismail,Al-Resayes, Saud I.,Siddiqui, M. Rafiq,Oves
, p. 1109 - 1119 (2013)
A new series of PdII complexes derived from thiosemicarbazone has been synthesized. The synthesized PdII complexes have been characterized on the basis of elemental analyses, FT-IR, 1H- and 13C-NMR, UV/VIS, and thermal studies. A square-planar geometry has been assigned around PdII ions on the basis of results obtained from UV/VIS studies. The thiosemicarbazone ligand and its PdII complexes have been screened against Gram-positive (Bacillus subtilis and Staphylococcus aureus) and Gram-negative (Escherichia coli and Pseudomonas aeruginosa) bacteria in vitro as growth-inhibiting agents, and the results revealed significant antibacterial activities. Copyright
Novel iron carbonyl complexes from thiophene-2-carboxaldehyde thiosemicarbazone
Hong, Wen-Shyan,Wu, Chih-Yu,Lee, Chen-Shiang,Hwang, Wen-Shu,Chiang, Michael Y.
, p. 277 - 285 (2004)
The reaction of thiophene-2-carboxaldehyde thiosemicarbazone (2-C4H3SCHNNHC(S)NH2) (1) with diiron nonacarbonyl under mild conditions in anhydrous benzene yields three iron carbonyl organometallic clusters: (i) Fe2S2 square-base pyramidal cluster 2 ([Fe(CO)3]3(μ3-S)2), (ii) Fe2S2 square-base pyramidal metal carbene cluster 3 ([Fe(CO)3]2Fe(CO)2 (μ3-S)2(C(NH2)NHNCH (2-C4H3S)), and (iii) double butterfly cluster 4 ([Fe(CO)3]3Fe(CO)2(μ4-S) (C,N; C(NH2)NHNCH(2-C4H3S) (μ2-S, N; SC(NH2)NNCH(2-C4 H3S)), and an octahedral complex 5 (Fe(CO)2(S, N; SC(NH2)NNCH (2-C4H3S))2. These products were fully characterized spectrally. The molecular structures of 1, 3, 4, and 5 have been determined by single-crystal X-ray diffraction.
Effect directed synthesis of a new tyrosinase inhibitor with anti-browning activity
Alonso, Victoria L.,Ayelen Ramallo, I.,Cabezudo, Ignacio,Furlan, Ricardo L. E.
, (2020/10/16)
The inhibition of enzymatic browning is an attractive target to elevate the quality of foods. The objective of this work is to describe a novel platform for the discovery of tyrosinase inhibitors, based on (a) one-pot preparation of a library of thiosemicarbazide compounds, (b) biological evaluation using tyrosinase TLC bioautography, (c) inhibitor identification via mass spectrometry coupled to bioautography. During these proof-of-concept experiments, the approach led to the straightforward identification of a new thiosemicarbazone with improved tyrosinase inhibition properties and fresh-cut apple slices antibrowning effect when compared to kojic acid. In conclusion, the platform represents an interesting strategy for the discovery of this type of inhibitors.
Thiosemicarbazones exhibit inhibitory efficacy against New Delhi metallo-β-lactamase-1 (NDM-1)
Ge, Ying,Kang, Peng-Wei,Li, Jia-Qi,Gao, Han,Zhai, Le,Sun, Le-Yun,Chen, Cheng,Yang, Ke-Wu
, p. 574 - 579 (2021/07/17)
The superbug infection caused by metallo-β-lactamases (MβLs) carrying drug-resistant bacteria, specifically, New Delhi metallo-β-lactamase (NDM-1) has become an emerging threat. In an effort to develop novel inhibitors of NDM-1, thirteen thiosemicarbazones (1a-1m) were synthesized and assayed. The obtained molecules specifically inhibited NDM-1, with an IC50 in the range of 0.88–20.2 μM, and 1a and 1f were found to be the potent inhibitors (IC50 = 1.79 and 0.88 μM) using cefazolin as substrate. ITC and kinetic assays indicated that 1a irreversibly and non-competitively inhibited NDM-1 in vitro. Importantly, MIC assays revealed that these molecules by themselves can sterilize NDM-producing clinical isolates EC01 and EC08, exhibited 78-312-fold stronger activities than the cefazolin. MIC assays suggest that 1a (16 μg ml?1) has synergistic antimicrobial effect with ampicillin, cefazolin and meropenem on E. coli producing NDM-1, resulting in MICs of 4-32-, 4-32-, and 4-8-fold decrease, respectively. These studies indicate that the thiosemicarbazide is a valuable scaffold for the development of inhibitors of NDM-1 and NDM-1 carrying drug-resistant bacteria.
