Synthesis, structure-activity relationship and molecular docking of 3-oxoaurones and 3-thioaurones as acetylcholinesterase and butyrylcholinesterase inhibitors.

The present study describes efficient and facile syntheses of varyingly substituted 3-thioaurones from the corresponding 3-oxoaurones using Lawesson's reagent and phosphorous pentasulfide. In comparison, the latter methodology was proved more convenient, giving higher yields and required short and simple methodology. The structures of synthetic compounds were unambiguously elucidated by IR, MS and NMR spectroscopy. All synthetic compounds were screened for their inhibitory potential against in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Molecular docking studies were also performed in order to examine their binding interactions with AChE and BChE human proteins. Both studies revealed that some of these compounds were found to be good inhibitors against AChE and BChE.

Efficient Synthesis of Novel N-[4-Methyl-3-(4-(5-phenyl-1,3,4-oxadiazol-2- yl)phenyl)thiazol-2(3H)-ylidene]benzamide Hybrid Ring System as Potential Antibacterial Agents.

BACKGROUND: Heterocyclic compounds display versatile biological applications, so the aim of this paper was to prepare biologically important heterocycles with enhanced bacterial resistance and to evaluate for their various structural features that are responsible for their biological properties. OBJECTIVE: The objective was to synthesize bacterial resistance compounds with enhanced antibacterial properties. METHODS: Ester moiety containing thiazole ring was converted into its hydrazide derivatives. These heterocyclic derivatives were cyclized into another ring oxadiazole; hence a hybrid ring system of two biologically active rings was prepared. RESULTS: All the synthesized compounds were characterized by spectroscopic techniques and were screened for their antibacterial potential; they possess significant antibacterial activities. CONCLUSION: New hybrid heterocyclic ring systems were synthesized by cyclization of hydrazide derivatives by adopting two step strategy in good yields. All the synthesized compounds were evaluated for their antioxidant activities; they showed moderate to significant activities. QSAR and Molecular docking studies were performed to determine the mode of interaction. Experimental and computational data is in accordance with the determined antibacterial activities.

Multifunctional Electrically Conductive Copper Electroplated Fabrics Sensitizes by In-Situ Deposition of Copper and Silver Nanoparticles.

In this study, we developed multifunctional and durable textile sensors. The fabrics were coated with metal in two steps. At first, pretreatment of fabric was performed, and then copper and silver particles were coated by the chemical reduction method. Hence, the absorbance/adherence of metal was confirmed by the deposition of particles on microfibers. The particles filled the micro spaces between the fibers and made the continuous network to facilitate the electrical conduction. Secondly, further electroplating of the metal was performed to make the compact layer on the particle- coated fabric. The fabrics were analyzed against electrical resistivity and electromagnetic shielding over the frequency range of 200 MHz to 1500 MHz. The presence of metal coating was confirmed from the surface microstructure of coated fabric samples examined by scanning electron microscopy, EDS, and XRD tests. For optimized plating parameters, the minimum surface resistivity of 67 Ω, EMI shielding of 66 dB and Ohmic heating of 118 °C at 10 V was observed. It was found that EMI SH was increased with an increase in the deposition rate of the metal. Furthermore, towards the end, the durability of conductive textiles was observed against severe washing. It was observed that even after severe washing there was an insignificant increase in electrical resistivity and good retention of the metal coating, as was also proven with SEM images.