205806-29-7Relevant academic research and scientific papers
A KHSO4 mediated facile synthesis of 2-amino-1,3,4-oxadiazole derivatives
Gan, Zongjie,Han, Lei,Hu, Xiangnan,Long, Binyu,Tang, Qiang,Tian, Binghua,Wang, Chenyu,Wang, Zifan,Wu, Yue,Yu, Yu
supporting information, (2021/08/18)
A novel, efficient and mild KHSO4 mediated synthesis for 2-amino-1,3,4-oxadiazoles has been established via the cyclodesulfurization of benzoylhydrazine and isothiocyanate derivatives in one pot. The reactions proceeded smoothly at room tempera
Synthesis of some 1,3,4-thiadiazole derivatives as inhibitors of Entamoeba histolytica
Siddiqui, Shadab Miyan,Salahuddin, Attar,Azam, Amir
, p. 1305 - 1312 (2013/04/10)
In the quest for potent anti-amoebic agents, some 1,3,4-thiadiazole derivatives were synthesized and characterized by spectral data. The purity of the compounds was confirmed by elemental analysis. All the compounds were screened in vitro against HM1:IMSS strain of Entamoeba histolytica by microdilution method. The results revealed that compounds 1 (IC50 = 0.670 μM), 3 (IC50 = 1.60 μM) and 8 (IC50 = 0.522 μM) had much better anti-amoebic activity than the reference drug metronidazole (IC50 = 1.80 μM). Further, cytotoxicity of the compounds having IC50 value less than metronidazole was assessed by MTT assay on human breast cancer MCF-7 cell line and all the compounds were found low cytotoxic in the concentration range of 2.5-250 μM. Preliminary results indicate that these three compounds (1, 3 and 8) may be subjected to further investigations and it may be hoped that the present study will stimulate efforts towards the development of novel effective anti-amoebic agents.
1,3,4-Thiadiazole derivatives. Synthesis, structure elucidation, and structure-antituberculosis activity relationship investigation
Oru?, El?in E.,Rollas, Sevim,Kandemirli, Fatma,Shvets, Nathaly,Dimoglo, Anatholy S.
, p. 6760 - 6767 (2007/10/03)
A series of 2,5-disubstituted-1,3,4-thiadiazoles were synthesized, the compounds structures were elucidated and screened for the antituberculosis activity against Mycobacterium tuberculosis H37Rv using the BACTEC 460 radiometric system. Among the tested compounds, 2-phenylamino-5-(4-fluorophenyl) -1,3,4-thiadiazole 22 showed the highest inhibitory activity. The relationships between the structures of compounds and their antituberculosis activity were investigated by the Electronic-Topological Method (ETM) and feed forward neural networks (FFNNs) trained with the back-propagation algorithm. As a result of the approach, a system of pharmacophores and anti-pharmacophores has been found that effectively separates compounds of the examination set into groups of active and inactive compounds. The system can be applied to the screening and design of new active compounds possessing skeletons similar to those used in the present study.
Evaluation of antimycobacterial and anticonvulsant activities of new 1- (4-fluorobenzoyl)-4-substituted-thiosemicarbazide and 5-(4-fluorophenyl)-4- substituted-2,4-dihydro-3H,1,2,4-triazole-3-thione derivatives
Gulerman,Rollas
, p. 691 - 695 (2007/10/03)
Some new 1-(4-fluorobenzoyl)-4-alkyl/arylthiosemicarbazide (2a-g), 5- (4-fluorophenyl)4-alkyl/aryl-2,4-dihydr-3H-1,2,4-triazole-3-thione (3a-g) derivatives, 3-(benzylthio)-5-(4-fluorophenyl)-4-phenyl-4H-1,2,4-triazole (3h) and 2-acetyl-5-(4-fluorophenyl)-
