Search results for "thiazole"
showing 10 items of 244 documents
PPARδ Modulation by GW501516: An Unsuccessful Exercise Mimetic.
2017
Thiazole–amino acids: influence of thiazole ring on conformational properties of amino acid residues
2021
Abstract Post-translational modified thiazole–amino acid (Xaa–Tzl) residues have been found in macrocyclic peptides (e.g., thiopeptides and cyanobactins), which mostly inhibit protein synthesis in Gram + bacteria. Conformational study of the series of model compounds containing this structural motif with alanine, dehydroalanine, dehydrobutyrine and dehydrophenylalanine were performed using DFT method in various environments. The solid-state crystal structure conformations of thiazole–amino acid residues retrieved from the Cambridge Structural Database were also analysed. The studied structural units tend to adopt the unique semi-extended β2 conformation; which is stabilised mainly by N–H⋯N…
Anticancer properties of 5Z-(4- fuorobenzylidene)-2-(4- hydroxyphenylamino)-thiazol-4-one
2019
Abstract4-thiazolidinones, which are privileged structures in medicinal chemistry, comprise the well-known class of heterocycles and are a source of new drug-like compounds. Undoubtedly, the 5-bulky-substituted-2,4-thiazolidinediones - a class of antihyperglycemic glitazones, which are peroxisome proliferator-activated receptor gamma (PPARγ) agonists, are the most described group among them. As there are various chemically distinct 4-thiazolidinones, different subtypes have been selected for studies; however, their main pharmacological profiles are similar. The aim of this study was to evaluate the anticancer activity of 5Z-(4-fluorobenzylidene)-2-(4-hydroxyphenylamino)-thiazol-4-one (Les-2…
New Thiazole Nortopsentin Analogues Inhibit Bacterial Biofilm Formation.
2018
New thiazole nortopsentin analogues were conveniently synthesized and evaluated for their activity as inhibitors of biofilm formation of relevant Gram-positive and Gram-negative pathogens. All compounds were able to interfere with the first step of biofilm formation in a dose-dependent manner, showing a selectivity against the staphylococcal strains. The most active derivatives elicited IC50 values against Staphylococcus aureus ATCC 25923, ranging from 0.40&ndash
Antiviral Properties of Chemical Inhibitors of Cellular Anti-Apoptotic Bcl-2 Proteins
2017
Viral diseases remain serious threats to public health because of the shortage of effective means of control. To combat the surge of viral diseases, new treatments are urgently needed. Here we show that small-molecules, which inhibit cellular anti-apoptotic Bcl-2 proteins (Bcl-2i), induced the premature death of cells infected with different RNA or DNA viruses, whereas, at the same concentrations, no toxicity was observed in mock-infected cells. Moreover, these compounds limited viral replication and spread. Surprisingly, Bcl-2i also induced the premature apoptosis of cells transfected with viral RNA or plasmid DNA but not of mock-transfected cells. These results suggest that Bcl-2i sensiti…
CCDC 1935935: Experimental Crystal Structure Determination
2020
Related Article: Rakesh Puttreddy, J. Mikko Rautiainen, Toni Mäkelä, Kari Rissanen|2019|Angew.Chem.,Int.Ed.|58|18610|doi:10.1002/anie.201909759
CCDC 1935934: Experimental Crystal Structure Determination
2020
Related Article: Rakesh Puttreddy, J. Mikko Rautiainen, Toni Mäkelä, Kari Rissanen|2019|Angew.Chem.,Int.Ed.|58|18610|doi:10.1002/anie.201909759
CCDC 868802: Experimental Crystal Structure Determination
2012
Related Article: A.Cornia, F.Felluga, V.Frenna, F.Ghelfi, A.F.Parsons, M.Pattarozzi, F.Roncaglia, D.Spinelli|2012|Tetrahedron|68|5863|doi:10.1016/j.tet.2012.04.117
Associations Among Psychologically Controlling Parenting, Autonomy, Relatedness, and Problem Behaviors During Emerging Adulthood.
2017
ABSTRACTThe present study aimed to investigate the relations among perceived parental psychological control (PPC), autonomy and relatedness, and negative outcomes during emerging adulthood in two cultural contexts: Italy and the USA. More specifically, we explored the mechanisms through which dependency-oriented PPC (DPPC) and achievement-oriented PPC (APPC) are associated with both internalizing and externalizing difficulties, focusing on the mediating role of autonomy and relatedness. Participants were 418 European-American and 359 Italian college students. Results indicated that the expressions of PPC with regard to dependency and achievement were related to emerging adults’ negative out…
Quizartinib versus salvage chemotherapy in relapsed or refractory FLT3-ITD acute myeloid leukaemia (QuANTUM-R): a multicentre, randomised, controlled…
2019
Background Patients with relapsed or refractory FLT3 internal tandem duplication (FLT3-ITD)-positive acute myeloid leukaemia have a poor prognosis, including high frequency of relapse, poorer response to salvage therapy, and shorter overall survival than those with FLT3 wild-type disease. We aimed to assess whether single-agent quizartinib, an oral, highly potent and selective type II FLT3 inhibitor, improves overall survival versus salvage chemotherapy. Methods QuANTUM-R is a randomised, controlled, phase 3 trial done at 152 hospitals and cancer centres in 19 countries. Eligible patients aged 18 years or older with ECOG performance status 0-2 with relapsed or refractory (duration of first …