1752-30-3Relevant articles and documents
Growth dynamics and molecular structural analysis of Dimethylketo thiosemicarbazone single crystals for frequency conversion applications - Optical and thermal characterization
Sakunthaladevi,Jothi
, (2021)
New organic Schiff base of Dimethylketo thiosemicarbazone (DMKT) was synthesized by condensation process and grown by solvent slow evaporation method in methanol solution. The grown crystal was subjected to a single crystal and powder X-ray diffraction study and to identify that the material crystallized into a triclinic crystal system with a P-1 noncentrosymmetric space group. The X-Ray data reveals that the crystalline network cohesion of this compound. The FT-IR and FT Raman spectral analysis show the vibration behavior of chemical bonds in the grown material. Its optical behavior was examined by UV–VIS spectrum and the DMKT crystal was found to have transparency in the region between 350 nm and 1100 nm. The luminescent emission of the grown material was identified from the fluorescence spectrum. Improvement in the second harmonic generation efficiency of the grown material was studied by the Kurtz and Perry powder method and it shows 26.7 mV of green light emission. The thermal stability and melting point of DMKT were confirmed by various thermal analyses.
Synthesis and antimicrobial activities of novel 6-(1,3-thiazol-4-yl)-1,3- benzoxazol-2(3H)-one derivatives
Laczkowski, Krzysztof Z.,Misiura, Konrad,Biernasiuk, Anna,Malm, Anna,Grela, Izabela
, p. 41 - 46 (2014)
Synthesis, characterization and investigation of antimicrobial activities of seven new 6-(1,3-thiazol-4-yl)-1,3-benzoxazol-2(3H)-ones are presented. Their structures were determined using 1H NMR, 13C NMR and elemental analyses. The compounds possess some biological activity against Gram-positive bacteria, especially against Micrococcus luteus belonging to opportunistic pathogens, with an MIC of 31.25 μg/mL.
Novel 1,3-thiazolidin-4-one derivatives as promising anti- Candida agents endowed with anti-oxidant and chelating properties
Secci, Daniela,Carradori, Simone,Bizzarri, Bruna,Chimenti, Paola,De Monte, Celeste,Mollica, Adriano,Rivanera, Daniela,Zicari, Alessandra,Mari, Emanuela,Zengin, Gokhan,Aktumsek, Abdurrahman
, p. 144 - 156 (2016)
Pursuing our recent outcomes regarding the antifungal activity of N-substituted 1,3-thiazolidin-4-ones, we synthesized thirty-six new derivatives introducing aliphatic, cycloaliphatic and heteroaromatic moieties at N1-hydrazine connected with C2 position of the thiazolidinone nucleus and functionalizing the lactam nitrogen with differently substituted (NO2, NH2, Cl and F) benzyl groups. These compounds were tested to evaluate their minimum inhibitory concentration (MIC) against several clinical Candida spp. with respect to topical and systemic reference drugs (clotrimazole, fluconazole, ketoconazole, miconazole, tioconazole, amphotericin B). Moreover, anti-oxidant properties were also evaluated by using different protocols including free radical scavenging (DPPH and ABTS), reducing power (CUPRAC and FRAP), metal chelating and phosphomolybdenum assays. Moreover, for the most active derivatives we assessed the toxicity (CC50) against Hep2 human cells in order to characterize them as multi-target agents for fungal infections.
Unusual chemical transformations of acetone thiosemicarbazone mediated by ruthenium: C-H bond activation, thiolation, and C-N bond cleavage
Paul, Piyali,Seth, Dipravath Kumar,Richmond, Michael G.,Bhattacharya, Samaresh
, p. 1432 - 1440 (2014)
Upon reaction with Ru(PPh3)3Cl2 in ethanol in the presence of triethylamine, acetone thiosemicarbazone undergoes several interesting chemical transformations, such as thiolation via methyl C-H bond activation, C-N bond cleavage, and conversion of the CS fragment to CO. Two complexes (1 and 2) were obtained from this reaction, both of which contained a modified thiosemicarbazone coordinated in SNS- or SNO-mode, two triphenylphosphines and a N-bound thiocyanate. The crystal structures of both the complexes have been determined. Theoretical and mass spectral studies have been carried out to probe the transformations. These complexes show intense absorptions in the visible and ultraviolet regions. Cyclic voltammetry on both the complexes show a reversible oxidation near 0.6 V vs. SCE, followed by an irreversible oxidation near 1.2 V vs. SCE. DFT calculations have been carried out to explain the electronic spectra, as well as the electrochemical observations.
Synthesis, spectra and crystal structure of two copper(I) complexes of acetonethiosemicarbazone
Lhuachan, Sanchai,Siripaisarnpipat, Sutatip,Chaichit, Narongsak
, p. 263 - 267 (2003)
The reaction of copper(I) chloride with acetonethiosemicarbazone (tscac) in a copper to tscac molar ratio of 1:2 forms the cationic complex [Cu(tscac)2]Cl (1). When the ratio of the copper to tscac was reduced to 1:1, a dimeric complex [Cu2Cl2(tscac)2]2 (2) was obtained. In complex 2, two CuCl2 species act as bridging groups between two Cu(tscac)2 moieties forming an eight-membered ring, whereas in complex 1, there is no CuCl2 moiety in the structure. In both complexes the copper(I) center is coordinated in a distorted tetrahedral geometry to two tscac groups through the sulfur and the imine nitrogen atom. In dimeric complex 2, the sulfur atom in each tscac ligand coordinates weakly to copper(I) in the CuCl2 moiety giving the distorted tetrahedral geometry. For the free ligand, the vc=s vibration at 789 cm-1 appears at lower energy than in complexes 1 and 2 (754 and 744 cm-1 respectively) indicating coordination at the sulfur atom. The complexes synthesized by either electrochemical or chemical methods are identical. ( Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003).
CHEMICAL ACTIVATORS OF NICOTINAMIDE MONONUCLEOTIDE ADENLYLY TRANSFERASE 2 (NMNAT2) AND USES THEREOF
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Page/Page column 22-23; 28; 32, (2020/06/22)
The present application relates to novel semicarbazones and thiosemicarbazones, to processes for preparing them, to pharmaceutical preparations comprising them, to the use of the novel semicarbazones and thiosemicarbazones for treatment and/or prophylaxis of diseases and to the use thereof for production of a medicament for treatment and/or prophylaxis of diseases, especially of neurodegeneration and age-associated diseases or conditions associated with NAD loss. The present application also provides a method for high throughput screening of NMNAT2 activators.
Expedient routes to 1,2,4-triazolinium salts
Fliri, Lukas,Partl, Gabriel,Gelbrich, Thomas,Nerdinger, Sven,Wurst, Klaus,Schottenberger, Herwig
, p. 593 - 610 (2020/01/31)
Concomitant S-alkylation and ketazonation of thiosemicarbazide in acetone eventually led to unanticipated ring closure and formation of (3-alkylthio)-1,2,4-triazolinium salts. This initial finding was complemented by employing another three representative aldehydes and ketones. Supplementarily, some respective intermediates have been isolated by stepwise synthetic procedures. In addition to the usual spectroscopic characterization, the structures of six 1,2,4-triazolinium heterocycles, as well as two unexpected by-products thereof have been characterized by single-crystal X-ray diffraction.
THIAZOLE DERIVATIVE AND APPLICATIONS
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Paragraph 0091-0092, (2019/04/16)
A thiazole derivative serving as a DHODH inhibitor, and applications thereof. The present invention specifically relates to a compound represented by formula I, a pharmaceutical composition containing the compound represented by formula (I), and applications of the compound in the preparation of drugs for treating diseases mediated by the DHODH or drugs for inhibiting the DHODH.
Design, synthesis and biochemical evaluation of novel multi-target inhibitors as potential anti-Parkinson agents
Carradori, Simone,Ortuso, Francesco,Petzer, Anél,Bagetta, Donatella,De Monte, Celeste,Secci, Daniela,De Vita, Daniela,Guglielmi, Paolo,Zengin, Gokhan,Aktumsek, Abdurrahman,Alcaro, Stefano,Petzer, Jacobus P.
, p. 1543 - 1552 (2017/11/27)
New 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives are proposed as dual-target-directed monoamine oxidase B (MAO-B) and acetylcholinesterase (AChE) inhibitors, as well as antioxidant agents, for the treatment of neurodegenerative disorders such as Parkinson's disease. Rational molecular design, target recognition and predicted pharmacokinetic properties have been evaluated by means of molecular modelling. Based on these properties, compounds were synthesized and evaluated in vitro as MAO-B and AChE inhibitors, and compared to the activities at their corresponding isozymes, monoamine oxidase A (MAO-A) and butyrylcholinesterase (BuChE), respectively. Anti-oxidant properties, potentially useful in the treatment of neurodegenerative disorders, have been also investigated in vitro. Among the evaluated compounds, three inhibitors may be considered as promising dual inhibitors of MAO-B and AChE, in vitro. MAO-B inhibition was also shown to be competitive and reversible for compound 19.
Morphological and: In vitro evaluation of programmed cell death in MCF-7 cells by new organoruthenium(II) complexes
Devagi,Reyhaneh,Dallemer,Jayakumar,Kalaivani,Prabhakaran
, p. 8620 - 8636 (2017/08/15)
Cyclopentadienyl ruthenium(ii) thiosemicarbazone complexes with the general formula [Ru(η5-C5H5)(Ac-tsc)PPh3]·Cl (1), [Ru(η5-C5H5)(Ac-mtsc)PPh3]·Cl (2), [Ru(η5-C5H5)(Ac-etsc)PPh3]·Cl (3) and [Ru(η5-C5H5)(Ac-ptsc)PPh3] (4) were synthesized and characterized by various spectroscopic techniques (1H NMR, 13C NMR, IR and UV-vis). The molecular structures of the representative complexes 2 and 4 were studied by single-crystal X-ray diffraction. The interactions of all the ligands and complexes with calf thymus DNA (CT-DNA) and bovine serum albumin (BSA) were studied using UV-vis and fluorescence emission spectroscopy. The results of binding studies revealed that the effective binding potentials of the complexes were higher than those of their parent ligands. All the new complexes 1-4 were investigated for their in vitro cytotoxic activity against MCF-7 human breast cancer cell line. All the complexes significantly inhibited cell proliferation in MCF-7 cells in a dose-dependent manner. Cytological observations via an inverted phase contrast microscope and a Hoechst 33342/PI dual-staining assay showed typical apoptotic morphology of cancer cells upon treatment with complexes 2 and 3. It can thus be suggested that the complexes 2 and 3 are modulated by apoptosis. The findings of the present study indicated that complexes 2 and 3 may become potent drugs for the treatment of cancer-related diseases only after further investigation.
