•Twenty six thiazole derivatives were designed and synthesized as a starting hits to be developed in the drug like molecules•Their in vitro anti-inflammatory activities have been screened in two ...assays•Compounds were screened in in vitro cell viability assays to evaluate potential cytotoxicity•Some screened compounds were found to be potent in the series by inhibiting LPS-induced TNFα release with IC50 values in µM range•One compound was found to be potent by inhibiting LPS-induced IL-8 release with IC50 values in µM range
Thiazoles are widely recognized as nuclei of great value for obtaining molecules with various biological activities, including analgesic, anti-inflammatory, anti-HIV, antidiabetic, antitumor and antimicrobial. A library of 26 thiazole derivatives as fragments were designed, synthesized and evaluated for their anti-inflammatory activities. Some screened compounds showed promising results and were found to be potent in the series by inhibiting LPS-induced TNFα and IL-8 release with IC50 values in µM range without cytotoxic activity.
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Flexible electronics is a new generation of electronic devices in which electronic components are integrated into flexible substrates. It is used in the fabrication of displays, solar cells, ...integrated circuits, and increasingly in the fabrication of electronic skin (E-skin), which can mimic the properties of human skin by being able to follow skin movements and flexures without loss of mechanical and electrical properties. E-skin is suitable for integrating various sensors to monitor personal health. Conductive polymers are used in flexible electronics due to their electrical conductivity, low mass, and stability. However, their main disadvantage is their brittleness, which is why they don’t possess flexibility property without modification. Therefore, in this work, the conductive polymer poly(3,4-ethylenedioxythiophene) (PEDOT) was used as the main chain and the side branches of poly(acrylate-urethane) (PAU) were grafted onto it by atom transfer radical polymerization (ATRP) onto it, obtaining the grafted copolymer PEDOT-
-PAU. In this way, the main chain of PEDOT retains the property of electrical conductivity without losing conjugation, while the side branches of PAU have the ability to crosslink non-covalently through hydrogen bonds with PAU side branches of adjacent polymer molecules due to the presence of oxygen in their structure. The presence of hydrogen bonds allows increasing the stretchability and flexibility of the material, and they also have the ability to spontaneously renew themselves when they break due to excessive stress. Three different synthesis conditions were used to obtain polymers of different structure, which were characterized by Fourier transform infrared spectroscopy (FTIR), nuclear magnetic resonance (NMR), scanning electron microscopy (SEM), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC) and measurement of electrical conductivity with a four-point probe (4PP) method. The obtained graft copolymer was prepared in the form of ink and printed on a polyurethane (PU) substrate using inkjet technique. The conductivity of the printed layer, its elongation and adhesion were investigated, while possible delamination of the printed polymer layer was also monitored. The results showed that the PEDOT-
-PAU copolymer was successfully synthesized and inkjet printing on PU film was successful. The obtained material has satisfactory electrical and mechanical properties and could be used for the integration of fully functional biosensors with further optimization of the composition.
One of the most widely used conductive polymers in the growing conductive polymer industry is poly(3,4-ethylenedioxythiophene) (PEDOT), whose main advantages are good thermal and chemical stability, ...a conjugated backbone, and ease of functionalization. The main drawback of PEDOT for use as wearable electronics is the lack of stretchable and self-healing properties. This can be overcome by grafting PEDOT with flexible side branches. As pure PEDOT is highly stable and grafting would not be possible, a new bromine-functionalized thiophene derivative, 2-(tiophen-3-yl) ethyl 2-bromo-2-methylpropanoate (ThBr), was synthesized and copolymerized with EDOT for the synthesis of a poly(EDOT-co-ThBr) ATRP macroinitiator. After the synthesis of the macroinitiator, flexible polymers could be introduced as side branches by atom-transfer radical polymerization (ATRP) to modify mechanical properties. Before this last synthesis step, the conditions for the synthesis of the ATRP macroinitiator should be investigated, as only functionalized units can function as grafting sites. In this study, nine new copolymers with different monomer ratios were synthesized to investigate the reactivity of each monomer. The ratios used in the different syntheses were ThBr:EDOT = 1:0.2, 1:0.4, 1:0.6, 1:0.8, 1:1, 0.8:1, 0.6:1, 0.4:1, and 0.2:1. In order to determine the effect of reaction time on the final properties of the polymer, macroinitiator synthesis at a 1:1 ratio was carried out at different time periods: 8 h, 16 h, 24 h, and 48 h. The obtained products were characterized by different techniques, and it was found that polymerizations longer than 24 h yielded practically insoluble macroinitiators, thus limiting its further application. Reactivity ratios of both monomers were found to be similar and close to 1, making the copolymerization reaction symmetrical and the obtained macroinitiators almost random copolymers.
The aim of this study was to synthesize an intrinsically stretchable conductive polymer (CP) by atom transfer radical polymerization (ATRP). For this purpose, poly(3,4-ethyilenedioxythiophene) ...(PEDOT) was synthesized as a backbone, while poly(acrylate-urethane) (PAU) was grafted onto the PEDOT backbone to form graft polymers PEDOT-g-PAU. Different concentrations of acrylate-urethane (AU) were used to synthesize PAU side chains of different lengths. The successful synthesis of the obtained intermediates and products (PEDOT-g-PAU) was confirmed by infrared spectroscopy and nuclear magnetic resonance. Thermal properties were evaluated by differential scanning calorimetry and thermogravimetric analysis, while conductivity was determined by four-point probe measurement. A simple tensile test was performed to characterize the ductility of the samples. PEDOT-g-PAU has shown high stretchability of up to 500% and, therefore, could potentially be used in skin-worn flexible electronics, while additional subsequent doping is required to improve the deterioration of electrical properties after the addition of the insulating urethane layer.
Poli(3,4-etilendioksitiofen) (PEDOT) je elektrovodljivi polimer koji se primjenjuje u baterijama, superkondenzatorima, solarnim ćelijama i različitim biosenzorima u nosivoj elektronici. Kontroliranom ...radikalskom polimerizacijom prijenosom atoma (ATRP) moguće je cijepljenjem bočnih grana modificirati svojstava PEDOT-a za specifičnu primjenu. U ovom radu sintetizirani su ATRP makroinicijatori na osnovi PEDOT-a, funkcionalizirani reaktivnim bromom, koji omogućuje cijepljenje različitih polimera kao bočnih grana. Karakterizacija dobivenih uzoraka provedena je pomoću NMR-a, FTIR-a, GPC-a, TGA-a i mjerenjem elektrokemijskih svojstava. Pokazalo se da uzorak s manjim udjelom broma ima bolja kemijska svojstva i kao takav je prikladniji za daljnju sintezu i modifikaciju PEDOT-a.
In our previous research, some screened 1,3-thiazole fragments were found to be potent by inhibiting LPS-induced TNF$\alpha $ and IL-8 release with IC50 values in the $\mu $M range without cytotoxic ...activity. In the current study, 1,3-thiazole fragments were further investigated as potent cholinesterase inhibitors prompted by the previously documented anti-inflammatory effect of AChE inhibitors. Molecular docking enabled insight into stabilizing interactions between the selected thiazoles and the active site of AChE and BChE. According to these experimental results, the cholinesterase inhibitory and anti-inflammatory activity of 1,3-thiazoles were correlated and confirmed that the same compounds inhibited LPS-stimulated TNF$\alpha $ cytokine production in PBMCs and enzymes cholinesterases.
