133767-88-1Relevant articles and documents
Urease inhibitory kinetics, molecular docking, SAR and ADME studies of imine analogues
Imran, Aqeel,Iqbal, Jamshed,Naz, Asia,Qazi, Syeda Uroos
, p. 3512 - 3520 (2022/02/21)
A series of synthesized imine derivatives (3a-m), including thio-semicarbazone, semicarbazone, thiazole and oxazole functional moieties, were examined for in vitro urease inhibition activity. Among all the analogues, 3b, 3k and 3f were the most potent against urease, exhibiting IC50 values of 1.52 ± 0.026, 2.20 ± 0.018 and 2.94 ± 0.058 μM, respectively. Docking studies were performed for the potent inhibitors to demonstrate their binding interactions with urease. Kinetic studies were also performed to assess the mode of interaction of the most potent analogue with urease. Moreover, an in silico ADME study was performed to evaluate the drug likeness of the compounds. All the analogues showed favorable ADME profiles.
Novel one-pot expeditious synthesis of 2,4-disubstituted thiazoles through a three-component reaction under solvent free conditions
Sujatha, Kodam,Vedula, Rajeswar Rao
, p. 302 - 308 (2018/02/09)
An expeditious one pot method has been developed for the synthesis of 2,4-disubstituted thiazoles under solvent free conditions via a multicomponent approach. Substituted thiazoles were synthesized with high yields by the reaction of cyclic ketones, thios
MAOI activity of some novel series of substituted thiazol-2-yl-hydrazines
Mazzone,Pignatello,Panico,Mazzone,Puglisi,Pennisi,Raciti,Mazzone,Matera
, p. 902 - 910 (2007/10/02)
Three series of 2-thiazolylhydrazines were synthetized and evaluated for their MAO inhibitory (MAOI) activity, both by in vivo tests, to assay their influence on several MAOI activity-related parameters (the variation on blood pressure induced by tyramine