1516-37-6Relevant articles and documents
Search for the Active Ingredients from a 2-Aminothiazole DMSO Stock Solution with Antimalarial Activity
Ropponen, Henni-Karoliina,Bader, Chantal D.,Diamanti, Eleonora,Illarionov, Boris,Rottmann, Matthias,Fischer, Markus,Witschel, Matthias,Müller, Rolf,Hirsch, Anna K. H.
, p. 2089 - 2093 (2021)
Chemical decomposition of DMSO stock solutions is a common incident that can mislead biological screening campaigns. Here, we share our case study of 2-aminothiazole 1, originating from an antimalarial class that undergoes chemical decomposition in DMSO at room temperature. As previously measured biological activities observed against Plasmodium falciparum NF54 and for the target enzyme PfIspE were not reproducible for a fresh batch, we tackled the challenge to understand where the activity originated from. Solvent- and temperature-dependent studies using HRMS and NMR spectroscopy to monitor the decomposition led to the isolation and in vitro evaluation of several fractions against PfIspE. After four days of decomposition, we successfully isolated the oxygenated and dimerised compounds using SFC purification and correlated the observed activities to them. Due to the unstable nature of the two isolates, it is likely that they undergo further decomposition contributing to the overall instability of the compound.
Scalable synthesis and antibacterial evaluation of 2-(3-(N-(substituted phenyl)sulfamoyl)ureido)benzothiazoles
Cheraiet, Zinelaabidine,Meliani, Saida,Nessaib, Mounir,Hessainia, Sihem,Boukhari, Abbas,Djahoudi, Abdelghani,Regainia, Zine
, (2019/08/12)
A new series of 2-(3-(N-(substituted phenyl)sulfamoyl)ureido)benzothiazoles was synthesized via a one-pot efficient and scalable method, involving the condensation of 2-aminobenzothiazoles derivatives, substituted anilines, and chlorosulfonyl isocyanate. The products were obtained in good yield with a simple workup, and their structures were confirmed from their spectral analyses. The synthesized compounds were further screened for their antibacterial activity against Gram-positive and Gram-negative pathogenic strains. The molecules show promising activity in the MIC value range of 2–0.25 μg/ml against selected bacterial strains, especially against nonfermentative carbapenem-resistant bacteria (Pseudo VIM-2 and Acinetobacter baumanni).
BENZOTHIAZOLE DERIVATIVE AND ANTI-TUMOR USE THEREOF
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Paragraph 0021; 0025; 0026, (2016/05/10)
The present invention relates to a benzothiazole derivative of formula 1 or a pharmaceutically acceptable salt thereof and a process for preparation thereof. The present invention also relates to a pharmaceutical composition comprising the compounds and the use of the compounds in the preparation of an anti-tumor medicament.