247225-84-9Relevant articles and documents
Synthesis, crystal structures, and biological activity of zinc(II) complexes derived from 2-amino-1,3,4-thiadiazole derivatives
Zhu, Hui-Long,Liu, Yu-Wei,Tang, Zong-Ming,Yin, Fu-Jun,Liu, Wei-Wei,Cao, Zhi-Ling,Bao, Juan,Li, Meng,Qin, Ling-Yan,Shi, Da-Hua
, p. 78 - 81 (2017)
Two new similar zinc(II) complexes, [ZnCl2L12] and [ZnCl2L22], derived from the 2-amino-1,3,4-thiadiazole derivatives, were prepared and structurally characterized by X-ray diffraction. The Zn atom in each complex has a tetrahedral coordination and is coordinated by two N atoms of the ligands and two Cl atoms. The urease inhibitory activities of the complexes and the ligands were evaluated.
Novel 2-amino-1,3,4-thiadiazoles and their acyl derivatives: Synthesis, structural characterization, molecular docking studies and comparison of experimental and computational results
Er, Mustafa,Isildak, Gamze,Tahtaci, Hakan,Karakurt, Tuncay
, p. 102 - 113 (2016)
This study aims to synthesize and characterize compounds containing 2-amino-1,3,4-thiadiazole and compare experimental results to theoretical results. For this purpose, firstly mono, di and tetra 2-amino-1,3,4-thiadiazole compounds (2a-c, 14, 20 and 25) w
Novel Substituted Imidazo[2,1-b][1,3,4]Thiadiazole Derivatives: Synthesis, Characterization, Molecular Docking Study, and Investigation of Their In Vitro Antifungal Activities
Er, Mustafa,Tahtaci, Hakan,Karakurt, Tuncay,Onaran, Abdurrahman
, p. 2555 - 2570 (2019)
In this study, a new series of substituted imidazo[2,1-b][1,3,4]thiadiazole derivatives were synthesized. To this end, first 2-amino-1,3,4-thiadiazole derivatives (compounds 2a and 2b), the starting materials, were synthesized with high yields (82% and 79%, respectively). Then imidazo[2,1-b][1,3,4]thiadiazole derivatives (4–16), the target compounds, were synthesized from reactions of 2-amino-1,3,4-thiadiazole derivatives (2a and 2b) with 2-bromoacetophenone derivatives (3a–3i) (in yields of 52% to 71%). All of the synthesized compounds were characterized by 1H NMR, 13C NMR, Fourier transform infrared, elemental analysis, mass spectroscopy, and X-ray diffraction analysis (compounds 4–12, 14, and 15) techniques. In vitro antifungal activity tests were performed for all of the synthesized compounds. Inhibition zones, percentage of inhibition, minimum fungicidal activity, minimum inhibitory concentration, and lethal dose values of the target compounds were determined against some plant pathogens. According to the results of the biological activity tests, all of the synthesized compounds showed moderate to high levels of antifungal activity. Theoretical calculations were performed to support the experimental results. The geometric parameters of selected compounds (5, 6, and 8) were optimized using the density functional theory B3LYP/6-31G(d) method in the Gaussian 09W package program, and the frontier molecular orbitals (highest occupied molecular orbital–lowest unoccupied molecular orbital) were calculated theoretically. Finally, molecular docking studies were performed for antifungal activity studies of the selected compounds and to determine whether or not these compounds could be inhibitor agents for the 2RKV protein structure.
Gamma-glutamyl transpeptidase inhibitors and methods of use
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Page/Page column 4; 27, (2017/01/31)
Compositions that are effective in inhibiting gamma-glutamyl transpeptidase are disclosed. Methods of producing and using these compositions are also disclosed.
Divergent effects of compounds on the hydrolysis and transpeptidation reactions of γ-glutamyl transpeptidase
Wickham, Stephanie,Regan, Nicholas,West, Matthew B.,Kumar, Vidya Prasanna,Thai, Justin,Li, Pui Kai,Cook, Paul F.,Hanigan, Marie H.
experimental part, p. 476 - 489 (2012/09/22)
A novel class of inhibitors of the enzyme γ-glutamyl transpeptidase (GGT) were evaluated. The analog OU749 was shown previously to be an uncompetitive inhibitor of the GGT transpeptidation reaction. The data in this study show that it is an equally potent uncompetitive inhibitor of the hydrolysis reaction, the primary reaction catalyzed by GGT in vivo. A series of structural analogs of OU749 were evaluated. For many of the analogs, the potency of the inhibition differed between the hydrolysis and transpeptidation reactions, providing insight into the malleability of the active site of the enzyme. Analogs with electron withdrawing groups on the benzosulfonamide ring, accelerated the hydrolysis reaction, but inhibited the transpeptidation reaction by competing with a dipeptide acceptor. Several of the OU749 analogs inhibited the transpeptidation reaction by slow onset kinetics, similar to acivicin. Further development of inhibitors of the GGT hydrolysis reaction is necessary to provide new therapeutic compounds.
Microwave-assisted synthesis and antimicrobial activity of some imidazo[2,1-b][1,3,4]thiadiazole derivatives
Dhepe, Sharad,Kumar, Sujeet,Vinayakumar,Ramareddy, Sureshbabu A.,Karki, Subhas S.
, p. 1550 - 1556 (2012/11/07)
A simple and efficient method was developed for the synthesis of 2,6-disubstituted-imidazo[2,1-b][1,3,4] thiadiazoles under microwave (MW) activation using 2-amino-5-substituted-1,3,4-thiadiazoles and appropriate bromo ketones as materials. All reactions
