4334-74-1Relevant articles and documents
Spectroscopic and biological approach of Ni(II), Cu(II) and Co(II) complexes of 4-methoxy/ethoxybenzaldehyde thiosemicarbazone glyoxime
Babahan, Ilknur,Eyduran, Fatih,Coban, Esin Poyrazoglu,Orhan, Nil,Kazar, Didem,Biyik, Halil
, p. 205 - 215 (2014)
Two novel vicinal dioxime ligands containing (4-methoxybenzaldehyde thiosemicarbazone glyoxime (L1H2) or 4-ethoxybenzaldehyde thiosemicarbazone glyoxime (L2H2)) thiosemicarbazone units were synthesized and characterized using 1H NMR, 13C NMR, HMQC, MS, infrared and, UV-VIS. spectroscopy, elemental analysis, and magnetic susceptibility measurements. Mononuclear nickel(II), copper(II) and cobalt(II) complexes with a metal:ligand ratio of 1:2 for L1H2 and L2H2 were also synthesized. The effect of pH and solvent on the absorption spectra of both ligands and complexes was determined. IR spectra show that the ligands act in a bidentate manner and coordinates N 4 donor groups of the ligands to NiII, CuII and CoII ions. The detection of H-bonding (O-H?O) in the [M(LH)2] metal complexes by IR spectra supported the square-planar MN4 coordination of mononuclear complexes. The antimicrobial activities of compounds L1H2, L2H2, and their Ni(II), Cu(II) and Co(II) complexes were evaluated using the disc diffusion method against 12 bacteria and 4 yeasts. The minimal inhibitory concentrations (MICs) against 7 bacteria and 3 yeasts were also determined. Among the test compounds attempted, L1H2, [Ni(L 1H)2], [Cu(L1H)2], L 2H2, [Ni(L2H)2] and [Cu(L 2H)2] showed some activities against certain Gram-positive bacteria and some of the yeasts tested.
Synthesis and antityrosinase mechanism of benzaldehyde thiosemicarbazones: Novel tyrosinase inhibitors
Chen, Liang-Hua,Hu, Yong-Hua,Song, Wei,Song, Kang-Kang,Liu, Xuan,Jia, Yu-Long,Zhuang, Jiang-Xing,Chen, Qing-Xi
, p. 1542 - 1547 (2012)
p-Hydroxybenzaldehyde thiosemicarbazone (HBT) and p-methoxybenzaldehyde thiosemicarbazone (MBT) were synthesized and established by 1H NMR and mass spectra. Both compounds were evaluated for their inhibition activities on mushroom tyrosinase and free-cell tyrosinase and melanoma production from B16 mouse melanoma cells. Results showed that both compounds exhibited significant inhibitory effects on the enzyme activities. HBT and MBT decreased the steady state of the monophenolase activity sharply, and the IC50 values were estimated as 0.76 and 7.0 μM, respectively. MBT lengthened the lag time, but HBT could not. HBT and MBT inhibited diphenolase activity dose-dependently, and their IC50 values were estimated as 3.80 and 2.62 μM, respectively. Kinetic analyses showed that inhibition type by both compounds was reversible and their mechanisms were mixed-type. Their inhibition constants were also determined and compared. The research may supply the basis for the development of new food preservatives and cosmetic additives.
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
5-aryl-1-arylideneamino-1h-imidazole-2(3h)-thiones: Synthesis and in vitro anticancer evaluation
Abu Ali, Ola A.,Abu Almaaty, Ali H.,El-Sayed, El-Sherbiny H.,Fayad, Eman,Tantawy, Mohamed A. M.,Toson, Eslam E. M.,Zaki, Islam
, (2021/06/16)
A novel series of N-1 arylidene amino imidazole-2-thiones were synthesized, identified using IR,1H-NMR, and13C-NMR spectral data. Cytotoxic effect of the prepared compounds was carried out utilizing three cancer cell lines; MCF-7 breast cancer, HepG2 liver cancer, and HCT-116 colon cancer cell lines. Imidazole derivative 5 was the most potent of all against three cell lines. DNA flow cytometric analysis showed that, imidazoles 4d and 5 exhibit pre-G1 apoptosis and cell cycle arrest at G2/M phase. The results of the VEGFR-2 and B-Raf kinase inhibition assay revealed that compounds 4d and 5 displayed good inhibitory activity compared with reference drug erlotinib.
Effect of organic solvents on solvatochromic, fluorescence, and electrochemical properties of synthesized thiazolylcoumarin derivatives
Bahadur, Ali,Iqbal, Shahid,Ujan, Rabail,Channar, Pervaiz Ali,AL-Anazy, Murefah Mana,Saeed, Aamer,Mahmood, Qaiser,Shoaib, Muhammad,Shah, Mazloom,Arshad, Ifzan,Shabir, Ghulam,Saifullah, Muhammad,Liu, Guocong,Qayyum, Muhammad Abdul
, p. 1189 - 1197 (2021/04/16)
In this present investigation, thiazolylcoumarin derivatives (5a–5k) were synthesized from thiosemicarbazide, ethyl acetoacetate, and naphthaldehyde through a multistep route. The formation of thiazolylcoumarin derivatives with bioactive scaffolds was con
The design, synthesis, and: In vitro trypanocidal and leishmanicidal activities of 1,3-thiazole and 4-thiazolidinone ester derivatives
Haroon, Muhammad,De Barros Dias, Mabilly Cox Holanda,Santos, Aline Caroline da Silva,Pereira, Valéria Rêgo Alves,Freitas, Luiz Alberto Barros,Balbinot, Rodolfo Bento,Kaplum, Vanessa,Nakamura, Celso Vataru,Alves, Luiz Carlos,Brayner, Fábio André,Leite, Ana Cristina Lima,Akhtar, Tashfeen
, p. 2487 - 2500 (2021/01/29)
Chagas and leishmaniasis are both neglected tropical diseases, whose inefficient therapies have made them remain the cause for millions of deaths worldwide. Given this, we synthesized 27 novel 1,3-thiazoles and 4-thiazolidinones using bioisosteric and est
Synthesis of Emodin Amide Derivatives Containing 1,3,4-Thiadiazole and Their Inhibitory Activity on Vibrio harveyi
Cao, Lian-Gong,Cao, Zhi-Ling,Chen, Chao,Jiang, Kai-Jun,Liu, Shu-Hao,Liu, Wei-Wei,Ruan, Xin-Chi,Shao, Zhong-Bai,Shi, Da-Hua,Su, Zi-Qin,Wang, You-Xian,Wu, Yu-Ran,Wu, Yu-Yu
, p. 281 - 286 (2021/08/05)
A series of new 1,3,4-thiadiazole Emodin amide derivatives were synthesized through the connection of 5-substituted-1,3,4-thiadiazole-2-amine and Emodin carboxylic acids which were obtained by a two-step procedure starting from Emodin. Vibrio harveyi inhibition activities of the newly prepared compounds were evaluated. Results revealed that all compounds showed different degrees of inhibition on V. harveyi. Among them, compound 7a showed the best V. harveyi inhibition effect and the minimum inhibitory concentration (MIC) was 0.0625 mg/mL.
Compound containing thiosemicarbazone/semicarbazone structure and preparation method and medical application of compound
-
Paragraph 0198-0200; 0248-0250, (2020/08/25)
The invention belongs to the field of medicinal chemistry and pharmacotherapeutics, and particularly relates to compounds containing thiosemicarbazone/semicarbazone structures and a preparation methodand medical application of the compounds. The compound
Synthesis, spectral characterization and DNA interactions of 5-(4-substituted phenyl)-1,3,4-thiadiazol-2-amine scaffolds
Shivakumara,Murali Krishna
, (2019/09/18)
Five 5-(4-Substituted phenyl)-1, 3, 4-thiadiazole-2-amines have been prepared and structure of the compounds confirmed by spectroscopy studies. On the basis of spectroscopic studies, confirmed the formation of compounds. The DNA binding affinity of the prepared compounds was undertaken by absorption titration method and increasing the amount of CT-DNA observed hyperchromism or hypsochromism. The binding affinity compounds (except 5) are in the order of 4[13.341 × 104 M?1]>3 [8.505 × 104 M-1]>2 [3.567 × 104 M-1]>1[3.525 × 104 M?1]. The ethidiumbromide quenching results indicates CT-DNA was quenched by thiadiazoles via a static quenching mechanism. The DNA cleavage studies of the compounds were carried out in the presence and absence of H2O2 using gel electrophoresis experiment.
Synthesis of isothiosemicarbazones of potential antitumoral activity through a multicomponent reaction involving allylic bromides, carbonyl compounds and thiosemicarbazide
Assun??o, Laura S.,Bortoluzzi, Adailton J.,Creczynski-Pasa, Tania B.,Ferreira, Misael,Gouvêa, Daniela P.,Inaba, Juliana,Munaretto, Laiéli S.,Sá, Marcus M.
, (2020/05/06)
A convenient route for the synthesis of isothiosemicarbazones and 2-hydrazono-1,3-thiazin-4-ones through a multicomponent reaction featuring allylic bromides, carbonyl compounds and thiosemicarbazides is described. The transformations proceed under mild a
