50772-53-7Relevant academic research and scientific papers
Synthesis of some 2-[(benzazole-2-yl)thioacetylamino]thiazole derivatives and their antimicrobial activity and toxicity
Turan-Zitouni, Guelhan,Demirayak, Seref,Oezdemir, Ahmet,Kaplancikli, Zafer Asim,Yildiz, Mehmet Taha
, p. 267 - 272 (2004)
Some 2-[(benzazole-2-yl)thioacetylamino]thiazole derivatives (III) were synthesized by reacting 4-methyl-2-(chloroacetylamino)thiazole derivatives (I) with benzazol-2-thiole (II) in acetone in the presence of K2CO 3. The chemical structures of the compounds were elucidated by 1H NMR and FAB+-MS spectral data. The prepared compounds were tested for antimicrobial activity and toxicity.
COMBINATION THERAPY FOR TREATING MPS1
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Paragraph 0464-0465; 0466-0468; 0472-0474, (2021/08/14)
The application is directed to compounds of formula (I) and their salts and solvates, wherein B, R1, R2, R3, R3', R4, R4', and R5 are as set forth in the specification, as well as to methods for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or prevention of, e.g., MPS1, optionally in combination with α-L-iduronidase or an analog or variant thereof, e.g., laronidase.
Structure guided design and synthesis of furyl thiazolidinedione derivatives as inhibitors of GLUT 1 and GLUT 4, and evaluation of their anti-leukemic potential
Aguilera, Renato J.,Choe, Jun-yong,Hess, Jessica D.,Iancu, Cristina V.,Macias, Lucasantiago Henze,Meyer-Almes, Franz-Josef,Mrowka, Piotr,Ramaa, C. S.,Tilekar, Kalpana,Upadhyay, Neha
, (2020/07/07)
Cancer cells increase their glucose uptake and glycolytic activity to meet the high energy requirements of proliferation. Glucose transporters (GLUTs), which facilitate the transport of glucose and related hexoses across the cell membrane, play a vital ro
Synthesis and antimicrobial activity evaluation of new dithiocarbamate derivatives bearing thiazole/benzothiazole rings
Yurtta?, Leyla,?zkay, Yusuf,Duran, Murat,Turan-Zitouni, Gülhan,?zdemir, Ahmet,Cantürk, Zerrin,Kü?üko?lu, Kaan,Kaplanc?kl?, Zafer As?m
, p. 1166 - 1173 (2016/07/27)
The synthesis of 2-(substituted phenyl)-2-oxoethyl 4-(pyrimidin-2-yl)piperazin-1-carbodithiodate (A1-A24) derivatives and 2-(4-substituted thiazol-2-ylamino)-2-oxoethyl 4-(pyrimidin-2-yl)piperazin-1-carbodithiodate (B1-B14) derivatives was undertaken starting from the potassium salt of 4-(2-pyrimidinyl)piperazine dithiocarbamate. The structures of the obtained compounds were elucidated by1H NMR,13C NMR, MS spectral data, and elemental analysis. The antimicrobial activity of the thirty eight newly synthesized compounds were tested against 12 microorganism strains using the microdilution technique. Compounds 2-(4-ethoxycarbonylthiazol-2-ylamino)-2-oxoethyl 4-(pyrimidin-2-yl)piperazin-1-carbodithiodate (B12), 2-(3-fluorophenyl)-2-oxoethyl 4-(pyrimidin-2-yl)piperazin-1-carbodithiodate (A18) and 2-(3,4-difluorophenyl)-2-oxoethyl 4-(pyrimidin-2-yl)piperazin-1-carbodithiodate (A21) were determined to possess high antimicrobial activity.
Synthesis and antimicrobial evaluation of novel ethyl 2-(2-(4-substituted)acetamido)-4-subtituted-thiazole-5-carboxylate derivatives
Pawar, Chandrakant D.,Sarkate, Aniket P.,Karnik, Kshipra S.,Bahekar, Sushilkumar S.,Pansare, Dattatraya N.,Shelke, Rohini N.,Jawale, Chetan S.,Shinde, Devanand B.
, p. 3525 - 3528 (2016/07/21)
A series of novel molecules containing thiazole ring structure were designed and synthesized. The structures of the synthesized compounds were elucidated and confirmed by1H NMR,13C NMR, Mass spectrum and the purity was checked through HPLC analysis. Among these synthesized compounds, 3a–3i and 6a–6c were tested for their antimicrobial activity (minimum inhibitory concentration) against a series of strains of Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and against the strains of Candida albicans, Aspergillus flavus and Aspergillus niger for antifungal activity respectively. The results of the antimicrobial screening data revealed that most of the tested compounds showed moderate to good microbial inhibitions.
Design, synthesis and SAR exploration of tri-substituted 1,2,4-triazoles as inhibitors of the annexin A2-S100A10 protein interaction
Reddy, Tummala R.K.,Li, Chan,Guo, Xiaoxia,Fischer, Peter M.,Dekker, Lodewijk V.
, p. 5378 - 5391 (2014/12/11)
Recent target validation studies have shown that inhibition of the protein interaction between annexin A2 and the S100A10 protein may have potential therapeutic benefits in cancer. Virtual screening identified certain 3,4,5-trisubstituted 4H-1,2,4-triazoles as moderately potent inhibitors of this interaction. A series of analogues were synthesized based on the 1,2,4-triazole scaffold and were evaluated for inhibition of the annexin A2-S100A10 protein interaction in competitive binding assays. 2-[(5-{[(4,6-Dimethylpyrimidin-2-yl)sulfanyl]methyl}-4-(furan-2-ylmethyl)-4H-1,2,4-triazol-3-yl)sulfanyl]-N-[4-(propan-2-yl)phenyl]acetamide (36) showed improved potency and was shown to disrupt the native complex between annexin A2 and S100A10.
Synthesis and biological activity of thiazole dithiocarbamate derivatives
Gundogdu-Karaburun, Nalan
, p. 814 - 823 (2014/07/07)
In this study, we aimed at the synthesis of new 2-((5-substituted-4- methylthiazol-2-yl)amino)-2-oxoethyl 4- substitutedpiperazine-1-carbodithioate derivatives and their antibacterial, antifungal, antioxidant and AChE inhibitory evaluations. A set of fift
Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2- ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents
Apostolidis,Liaras,Geronikaki,Hadjipavlou-Litina,Gavalas,Sokovic,Glamoclija,Ciric
, p. 532 - 539 (2013/03/13)
As a part of our ongoing studies in developing new derivatives as dual antimicrobial/anti-inflammatory agents we describe the synthesis of novel 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones. All newly synthesized compounds were tested for
Synthesis of 2-[4,5-dimethyl-1-(phenylamino)-1H-imidazol-2-ylthio]-N- (thiazole-2-yl)acetamide derivatives and their anticancer activities
Duran, Murat,Demirayak, Seref
, p. 4110 - 4124 (2013/09/02)
In this work, 2-(4,5-dimethyl-1-(phenylamino)-1H-imidazol-2-ylthio)-N- (thiazol-2-yl) acetamide derivatives were synthesized by reacting 4,5-dimethyl-1-(phenylamino)-1H-imidazole-2(3H)-thione derivatives with some 2-chloro-N-(thiazol-2-yl)acetamide compou
Synthesis, physicochemical characterization, cytotoxicity, antimicrobial, anti-inflammatory and psychotropic activity of new N-[1,3-(benzo)thiazol-2-yl]- ω-[3,4-dihydroisoquinolin-2(1H)-yl]alkanamides
Zablotskaya, Alla,Segal, Izolda,Geronikaki, Athina,Eremkina, Tatiana,Belyakov, Sergey,Petrova, Marina,Shestakova, Irina,Zvejniece, Liga,Nikolajeva, Vizma
, p. 846 - 856 (2013/12/04)
A series of new N-[(benzo)thiazol-2-yl]-2/3-[3,4-dihydroisoquinolin-2(1H)- yl]ethan/propanamide derivatives was synthesized and characterized by 1H, 13C NMR and IR spectroscopy and mass-spectrometry. A single crystal X-ray study of N
