2929-81-9Relevant articles and documents
Facile synthesis of novel fluorescent thiazole coumarinyl compounds: Electrochemical, time resolve fluorescence, and solvatochromic study
Ahmad, Zahoor,Arshad, Ifzan,Bahadur, Ali,Channar, Pervaiz Ali,Iqbal, Shahid,Irfan, Rana Muhammad,Javed, Mohsin,Khalid, Bilal,Liu, Guocong,Mahmood, Qaiser,Qayyum, Muhammad Abdul,Raheel, Muhammad,Rizwan, Komal,Saeed, Aamer,Saifullah, Muhammad,Shabir, Ghulam,Shoaib, Muhammad,Ujan, Rabail
, (2021)
In this study, Benzocoumarin-Thiazoles-Azomethine derivatives with bioactive scaffolds were synthesized and characterized. The present investigation is concerned with the multistep synthesis of thiazole coumarinyl derivatives (5a-k), which were accomplished from naphthaldehyde, ethyl acetoacetate, and thiosemicarbazide. The formation of newly synthesized derivatives was confirmed by 1H NMR and 13C NMR spectroscopic studies. Thiazole coumarinyl derivatives were subjected to UV-Visible studies in different solvents such as ethanol, ethyl acetate, and DMF for solvatochromic studies. The synthesized coumarinyl thiazole compounds showed absorption in the range of 332-390 nm. Electrochemical studies were performed in DMSO and redox behavior was offered by thiazoles. Fluorescence of coumarinyl thiazole compounds were examined in ethanol, ethyl acetate, and DMF to visualize the solvent effect on the emitting ability of compounds. Fluorescence spectra of coumarinyl thiazoles expressed a sharp emission in the range 436-550 nm.
Adsorption and inhibitor action of 4-(N,N-dimethylamino) benzaldehyde thiosemicarbazone on 6061 Al/SiC composite and its base alloy in sulfuric acid medium
Pinto, Geetha Mable,Nayak, Jagannath,Shetty, A. Nityananda
, p. 127 - 140 (2011)
The inhibitive action of 4-(N,N-dimethylamino)benzaldehyde thiosemicarbazone (DMABT) on the corrosion behavior of 6061 Al -15 vol. pct. SiC(p) composite and its base alloy was studied at different temperatures in sulfuric acid medium containing varying co
Thiosemicarbazone Derivatives as Inhibitors of Amyloid-β Aggregation: Effect of Metal Coordination
Caballero, Ana B.,Espargaró, Alba,Gamez, Patrick,Lorenzo, Carmen,Matesanz, Ana I.,Quiroga, Adoración G.,Sabaté, Raimon
, (2020)
Three thiosemicarbazone derivatives, namely 4-(dimethylamino)benzaldehyde 4,4-dimethylthiosemicarbazone (HL1), 4-(dimethylamino)benzaldehyde thiosemicarbazone (HL2), and 4-(dimethylamino)benzaldehyde 4-methylthiosemicarbazone (HL3), have been synthesized and characterized. The three palladium(II) complexes 1-3 were prepared respectively from HL1, HL2, and HL3. The crystal structures of two coordination compounds, namely Pd(L2)2 (2) and Pd(L3)2 (3), were obtained, which showed the expected square-planar environment for the metal centers. The ligand HL3 and the Pd(II) complexes 1-3, which are stable in buffered solutions containing up to 5% DMSO, exhibit remarkable inhibitory properties against the aggregation of amyloid-β, reducing the formation of fibrils. HL1, HL3, 2, and 3 display IC50 values (i.e., the concentrations required to reduce Aβ fibrillation by 50%) below 1 μM, lower that of the reference compound catechin (IC50 = 2.8 μM). Finally, in cellulo studies with E. coli cells revealed that the palladium(II) compounds are significantly more efficient than the free ligands in inhibiting Aβ aggregation inside bacterial inclusion bodies, thus illustrating a beneficial effect of metal coordination.
Synthesis, antimicrobial and antioxidant evaluation with in silico studies of new thiazole Schiff base derivatives
Ahmed, Junaid Uddin,Al-Macktuf, Abdullah,Haque, Md. Aminul,Islam, Md. Din,Nishino, Hiroshi,Rahman, Mohammad Mostafizur,Shah, Md. Shahazada
, (2021/10/19)
A series of nineteen thiazole Schiff base derivatives 2a-2s were synthesized (Scheme 1) and elucidated by spectral analyses (IR, 1H NMR and HRMS). The evaluation of their antimicrobial activities against two gram-positive, two gram-negative, an
Design and efficient synthesis of novel 4,5-dimethylthiazole-hydrazone derivatives and their anticancer activity
Evren, Asaf Evrim,Yurtta?, Leyla,Ekselli, Bü?ra,Aksoy, Onur,Akalin-?ift?i, Gül?en
, p. 372 - 386 (2021/06/17)
Background: Recently, researchers have been warning about the increased mortality of the various cancer types. Also, the lung adenocarcinoma and the glioma types are burning issues for world's health due to late or wrong diagnosis and/or insufficient treatment methods. For this purpose, our research group designed and synthesized novel 4,5-dimethyl thiazole-hydrazone derivatives which were tested against cancer and normal cell lines to understand the structure-activity relationship (SAR). Methods: The lead compounds were obtained by reacting 2-(substituted aryl-2-ylmethylene) hydrazin-1-carbothioamide with 3-chloro-2-butanone derivatives. The structural elucidation of the compounds was performed by1H-NMR,13C-NMR, and LC/MS-IT-TOF spectral and elemental analyses. The synthesized compounds were tested in vitro for the anticancer activity against A549 human lung adenocarcinoma and C6 rat glioma cells and investigated for which pathway to induce cell death. Also, the docking study of the active compounds was achieved to understand the SAR. Results: The targeted compounds (2a-2l) were synthesized successfully above 70% yields, and the analysis findings proved their purity. In general, the results of activity studies displayed significant effects against at least one cell line, except compounds 2e (indol-3-yl) and 2h (4-dimethylaminophenyl). Furthermore, compounds 2b and 2f displayed potential anticancer activity. With the help of molecular docking study, a potential selectivity of compound 2f was observed for type II protein kinase. On the other hand, compound 2b interacted with the active site nearly the same as Dasatinib. Therefore, these two compounds could be used as a base on developing selective anticancer drugs. Conclusion: Pyridin-2-yl (2b) derivative was found to be a favorable molecule with high anticancer potency against C6 and A549 cell lines. Additionally, 1-naphthyl (2f) derivative was a worthy compound for potential selectivity. In future studies, it will be our priority to focus on developing derivatives of these two compounds (2b and 2f) and elucidate their mechanisms.
