21258-10-6Relevant 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.
supporting information, p. 2089 - 2093 (2021/05/10)
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.
Hirshfeld surface analysis of some new heteroleptic Copper(I) complexes
Mohd Zubir, Mohamad Zarif,Jamaludin, Nazzatush Shimar,Abdul Halim, Siti Nadiah
, p. 141 - 150 (2019/05/29)
Seven new coordination complexes namely, [Cu(T1) (I) (PPh3)2] (CT1), [Cu(T2) (I) (PPh3)2] (CT2), [Cu(T3) (I) (PPh3)2] (CT3), [Cu(T4) (I) (PPh3)2] (CT4), [Cu(T5) (I) (P
Synthesis of thiazolone derivatives as novel soybean 15-LOX inhibitors
Mahdavi, Mohammad,Saeedi, Mina,Nadri, Hamid,Eghtedari, Mohammad,Gholizadeh, Sama,Hariri, Roshanak,Akbarzadeh, Tahmineh
, p. 186 - 191 (2017/06/21)
Background: Thiazole derivatives are known as important sulfur containing heterocycles which are present in a wide range of biologically active natural products. Methods: A series of thiazolone derivatives were synthesized and evaluated for their soybean 15-LOX inhibitory activity. The title compounds were prepared by the reaction of 2-arylthiazol-4(5H)-ones and different aromatic aldehydes. All compounds were characterized and evaluated against soybean 15-LOX. Results: Among the synthesized thiazolone derivatives, 5-(4-methoxybenzylidene)-2-((2-methoxyphenyl) amino)thiazol-4(5H)-one (3l) was found to be the most active compound comparing with quercetin as the reference drug. Conclusion: It seems that prepared thiazolones having methoxy groups both on aryl and aminoaryl moieties can be considered for further drug discovery research.