533-02-8Relevant articles and documents
Synthesis, inhibition of mycobacterium tuberculosis enoyl-acyl carrier protein reductase and antimycobacterial activity of novel pentacyanoferrate(II)-isonicotinoylhydrazones
Gazzi, Thais P.,Rotta, Mariane,Villela, Anne D.,Rodrigues, Valn's,Martinelli, Leonardo K.B.,Sales, Francisco Adilson M.,Silva De Sousa, Eduardo Henrique,Campos, Maria Martha,Basso, Luiz Augusto,Santos, Diógenes S.,Machado, Pablo
, p. 2028 - 2037 (2017/09/01)
Tuberculosis remains among the top causes of death triggered by a single pathogen. Herein, a greener synthetic approach for isonicotinoylhydrazones is described using ultrasound energy. These compounds were used as starting materials for synthesizing pent
MFA zeotype catalyst: A greener approach for the synthesis of INH azomethine scaffolds
Raghuvanshi, Devendra S.,Mahulikar, Pramod P.,Meshram, Jyotsna S.
, p. 48071 - 48078 (2015/06/16)
Herein, we are reporting the green and efficient synthesis of some pharmacologically important azomethine derivatives of isoniazide (INH) using Modified Fly Ash (MFA) as an excellent zeotic solid acid catalyst. The catalyst, by virtue of its terminal hydr
Structure-based optimization of oxadiazole-based GSK-3 inhibitors
Lo Monte, Fabio,Kramer, Thomas,Gu, Jiamin,Brodrecht, Martin,Pilakowski, Johannes,Fuertes, Ana,Dominguez, Juan Manuel,Plotkin, Batya,Eldar-Finkelman, Hagit,Schmidt, Boris
, p. 26 - 40 (2013/04/23)
Inhibition of glycogen synthase kinase-3 (GSK-3) induces neuroprotective effects, e.g. decreases β-amyloid production and reduces tau hyperphosphorylation, which are both associated with Alzheimer's disease (AD). The two isoforms of GSK-3 in mammalians are GSK-3α and β, which share 98% homology in their catalytic domains. We investigated GSK-3 inhibitors based on 2 different scaffolds in order to elucidate the demands of the ATP-binding pocket [1]. Particularly, the oxadiazole scaffold provided potent and selective GSK-3 inhibitors. For example, the most potent inhibitor of the present series, the acetamide 26d, is characterized by an IC50 of 2 nM for GSK-3α and 17 nM for GSK-3β. In addition, the benzodioxane 8g showed up to 27-fold selectivity for GSK-3α over GSK-3β, with an IC 50 of 35 nM for GSK-3α. Two GSK-3 inhibitors were further profiled for efficacy and toxicity in the wild-type (wt) zebrafish embryo assay to evaluate simultaneously permeability and safety.