Search results for "thiazole"

Secondary nucleation and accessible surface in insulin amyloid fibril formation.

2008

At low pH insulin is highly prone to self-assembly into amyloid fibrils. The process has been proposed to be affected by the existence of secondary nucleation pathways, in which already formed fibrils are able to catalyze the formation of new fibrils. In this work, we studied the fibrillation process of human insulin in a wide range of protein concentrations. Thioflavin T fluorescence was used for its ability to selectively detect amyloid fibrils, by mechanisms that involve the interaction between the dye and the accessible surface of the fibrils. Our results show that the rate of fibrillation and the Thioflavin T fluorescence intensity saturate at high protein concentration and that, surpr…

N-Heterocyclic Carbene Catalyzed Asymmetric Synthesis of Dihydropyranothiazoles­ via Azolium Enolate Intermediates

2017

A highly diastereo- and enantiostereoselective synthesis of bicyclic dihydropyranothiazoles combining a thiazole and δ-lactone skeleton via NHC-catalyzed [4+2] annulation of 5-alkenylthiazolones and α-chloroaldehydes has been developed. The heterocyclic products are formed via azolium enolate intermediates in good yields with high diastereo- and enantistereoselectivities.

Interaction of metal ions with D-glucobenzothiazoline: isolation and characterization of the resultant products

2002

Six different metal-ion complexes of D-glucobenzothiazoline were synthesized and characterized by analytical and spectral techniques. Formation of different types of species (ML and ML2) were observed with Cu2+, Ag+, Cd2+, Hg2+, and Zn2+ ions. Existence of an anomeric mixture in the case of the Cu2+ complex is identified from the EPR spectra, and the results were further supported by the simulated spectra. The structures were proposed based on different studies.

Synthesis and anti-HIV activity of 2,3-diaryl-1,3-thiazolidin-4-ones

2002

Several 1,3-thiazolidin-4-ones bearing a 2,6-dihalophenyl group at C-2 and a variously substituted phenyl ring at N-3 have been synthesized and tested as anti-HIV agents. The results of the in vitro tests showed that some of them proved to be effective inhibitors of HIV-1 replication.

Synthesis of new 2,3-diaryl-1,3-thiazolidin-4-ones as anti-HIV agents

2004

Several 2,3-diaryl-1,3-thiazolidin-4-ones were synthesized and evaluated as anti-HIV agents. The results of the in vitro tests showed that some of them were highly effective inhibitors of HIV-1 replication at 30-50 nM concentrations with minimal cytotoxicity, thereby acting as non-nucleoside HIV-1 reverse transcriptase inhibitors (NNRTIs).

Polycyclic Pyrrolo-Thiazole Systems with Biological Activity

A Novel Series of Acylhydrazones as Potential Anti-Candida Agents: Design, Synthesis, Biological Evaluation and In Silico Studies

2019

In the context of an increased incidence of invasive fungal diseases, there is an imperative need of new antifungal drugs with improved activity and safety profiles. A novel series of acylhydrazones bearing a 1,4-phenylene-bisthiazole scaffold was designed based on an analysis of structures known to possess anti-Candida activity obtained from a literature review. Nine final compounds were synthesized and evaluated in vitro for their inhibitory activity against various strains of Candida spp. The anti-Candida activity assay revealed that some of the new compounds are as active as fluconazole against most of the tested strains. A molecular docking study was conducted in order to evaluate the …

Alternariol-induced cytotoxicity in Caco-2 cells. Protective effect of the phenolic fraction from virgin olive oil.

2014

The extra virgin olive oil (EVOO) has been associated to antioxidant effects. The mycotoxin alternariol (AOH) can contaminate olives. The aims of this work were to determine the cytotoxic effects and reactive oxygen species (ROS) produced by AOH, tyrosol and oleuropein (two polyphenols of olive oil) and a real EVOO extract in Caco-2 cells. The MTT assay and the ROS production by the H2-DCFDA probe were used. Results demonstrated that AOH reduces cellular proliferation depending on concentration, whereas tyrosol and oleuropein did not (12.5-100 μM). The combination of AOH + oleuropein (50 μM) increased cell proliferation (24%) whereas, AOH + tyrosol decreased (47%) it. Besides, AOH increased…

Measurement of interactions between polysaccharides and flavour compounds by exclusion size chromatography: Advantages and limits

1998

Interactions between flavour compounds and polysaccharides have been studied by exclusion size chromatography, the Hummel and Dreyer method. Hydrogen bonding was found between 2-acetyl thiazole and dextrines of different degrees of polymerisation. The number of binding sites and the affinity constant increase by increasing the degree of polymerisation. Hydrogen bonding was also responsible for the interactions between xanthane and 1-octen-3-ol or 2-acetyl pyrazine, with 1 mole of 1-octen-3-ol bound per pentasaccharide repeating unit. Unfortunately, the number of flavour compounds, which can be studied with this method, is limited due to their low water solubility and their low UV absorption.

Synthesis and Biological Properties of Benzothiazole, Benzoxazole, and Chromen-4-one Analogues of the Potent Antitumor Agent 2-(3,4-Dimethoxyphenyl)-…

2008

New fluorinated 2-aryl-benzothiazoles, -benzoxazoles, and -chromen-4-ones have been synthesized and their activity against MCF-7 and MDA 468 breast cancer cell lines compared with the potent antitumor benzothiazole 5. Analogues such as 9a, b and 12a, d yielded submicromolar GI50 values in both cell lines; however, none of the new compounds approached 5 in terms of antitumor potency. For 5, binding to the aryl hydrocarbon receptor appeared to be necessary but not sufficient for growth inhibition.