10445-04-2Relevant academic research and scientific papers
Synthesis and evaluation of 1,3,4-oxadiazole derivatives for development as broad-spectrum antibiotics
Tresse, Cédric,Radigue, Richard,Gomes Von Borowski, Rafael,Thepaut, Marion,Hanh Le, Hong,Demay, Fanny,Georgeault, Sylvie,Dhalluin, Anne,Trautwetter, Annie,Ermel, Gwennola,Blanco, Carlos,van de Weghe, Pierre,Jean, Micka?l,Giard, Jean-Christophe,Gillet, Reynald
, (2019/09/18)
The reality and intensity of antibiotic resistance in pathogenic bacteria calls for the rapid development of new antimicrobial drugs. In bacteria, trans-translation is the primary quality control mechanism for rescuing ribosomes arrested during translation. Because trans-translation is absent in eukaryotes but necessary to avoid ribosomal stalling and therefore essential for bacterial survival, it is a promising target either for novel antibiotics or for improving the activities of the protein synthesis inhibitors already in use. Oxadiazole derivatives display strong bactericidal activity against a large number of bacteria, but their effects on trans-translation were recently questioned. In this work, a series of new 1,3,4-oxadiazole derivatives and analogs were synthesized and assessed for their efficiency as antimicrobial agents against a wide range of gram-positive and gram-negative pathogenic strains. Despite the strong antimicrobial activity observed in these molecules, it turns out that they do not target trans-translation in vivo, but they definitely act on other cellular pathways.
SUBSTITUTED PYRAZOLE COMPOUNDS AND METHODS OF USING THEM FOR TREATMENT OF HYPERPROLIFERATIVE DISEASES
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Paragraph 260, (2018/06/21)
Disclosed are compounds useful, for example, in methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for
2-(4-trifluoromethylphenyl)-6-ferrocenyl-imidazo[2,1-b]-1,3,4-thiadiazole preparation method
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Paragraph 0022; 0023; 0024; 0025; 0026; 0027; 0037, (2018/01/12)
The present invention discloses a 2-(4-trifluoromethylphenyl)-6-ferrocenyl-imidazo[2,1-b]-1,3,4-thiadiazole preparation method, which comprises: carrying out stirring mixing on 2-amino-5-(4-trifluoromethylphenyl)-1,3,4-thiadiazole, alpha-bromo-acetylferrocene and ethanol; placing the mixed solution in a microwave oven, and carrying out microwave irradiation; after the alpha-bromo-acetylferrocene completely reacts, carrying out a microwave reaction; adding water to the reaction solution, and adjusting the pH value of the reaction solution to 7-8 with a saturated sodium carbonate solution; carrying out suction filtration, washing the filter cake with water, and drying to obtain a crude product; and re-crystallizing with DMF to obtain the target product. According to the present invention, the microwave-assisted synthesis reaction is used so as to substantially shorten the reaction time and improve the reaction efficiency.
Improved antiproliferative activity of 1,3,4-thiadiazole-containing histone deacetylase (HDAC) inhibitors by introduction of the heteroaromatic surface recognition motif
Guan, Peng,Wang, Lei,Hou, Xuben,Wan, Yichao,Xu, Wenfang,Tang, Weiping,Fang, Hao
, p. 5766 - 5775 (2015/02/02)
A series of 1,3,4-thiadiazole-containing hydroxamic acids, in accord with the common pharmacophore of histone deacetylase (HDAC) inhibitors (a Zn2+ binding moiety-a linker-a surface recognition motif), was identified as submicromolar HDAC inhibitors by our group. In this study, we continued our efforts to develop 1,3,4-thiadiazole bearing hydroxamate analogues by modifying the surface recognition motif. We found that 1,3,4-thiadiazoles having a heteroaromatic substituent showed better HDAC inhibitory activity in enzymatic assay and higher antiproliferative potency in cellular assay compared to SAHA.
Antihypertensive Thiadiazoles. 1. Synthesis of Some 2-Aryl-5-hydrazino-1,3,4-thiadiazoles with Vasodilator Activity
Turner, Stephen,Myers, Malcolm,Gadie, Brian,Nelson, Anthony J.,Pape, Robin,et al.
, p. 902 - 906 (2007/10/02)
Some 2-Aryl-5-hydrazino-1,3,4-thiadiazoles have been synthesized and screened for antihypertensive activity.In general, compounds with a 2-substituted phenyl ring had higher activity than their 3- or 4-substituted counterparts or those containing heteroar
A Convenient and General Synthesis of 2-Amino-1,3,4-thiadiazoles. Dehydration of Acylthiosemicarbazides with Methanesulfonic Acid
Kress, Thomas J.,Costantino, Silvio M.
, p. 607 - 608 (2007/10/02)
2-Amino-5-alkyl and 2-amino-5-aryl-1,3,4-thiadiazoles were prepared by the dehydration of 2-acylthiosemicarbazides with molar equivalents of methanesulfonic acid in refluxing toluene.The synthesis appears to be general.
