Drugs can be delivered by a temperature change-driven shrinking of the nanocarrier followed by the cargo release. This paper describes a different structural response to temperature, performed by nanoparticles of poly(N-isopropylacrylamide) and hyaluronic acid. Around 35 °C, the hydrophobicity of the vinyl polymer drives a core-shell rearrangement with the acrylamide chains confined in the core and the polysaccharide moiety forming the shell.
View Article and Find Full Text PDFCombined reversible addition-fragmentation chain transfer (RAFT) and chemoselective "click" chemistry are used for assembling two polymeric chains into a hybrid network capable to respond simultaneously or separately to different external stimuli. An azido-derivative of hyaluronate is clicked together with a new telechelic RAFT-generated p(NiPAAm), carrying a propargyl function at both ends, suitable as macromolecular "clickable" cross-linker with controlled molecular weight. This hybrid system displays a multiresponsive behavior versus temperature, pH, and ionic strength, maintaining cumulative as well as separate sensitivities to the external stimuli.
View Article and Find Full Text PDFA new series of fluoro substituted pyrazoline derivatives 5a-g and 6a-g were synthesized in good to excellent yield from the corresponding pyrazole chalcones, 4a-g, by using polyethylene glycol-400 (PEG-400) as an alternative reaction medium. The newly synthesized compounds were characterized and screened for their in vivo antiinflammatory and analgesic activity. Compounds 5g and 6g were found to be more potent than standard drug Diclofenac and six other compounds 5b, 5c, 5f, 6b, 6c and 6f showed significant antiinflammatory activity as compared to standard drug.
View Article and Find Full Text PDFSynthesis of new 2-chloro-3-((4-phenyl-1H-1,2,3-triazol-1-yl)methyl)quinoline derivatives (4a-h) using 1,3-dipolar cycloaddition (click chemistry) reaction of 3-(azidomethyl)-2-chloro-quinoline derivatives (3a-h) with phenyl acetylene in the presence of Cu(I) catalyst has been achieved in very high yield. These molecules were evaluated in vitro for their antifungal and antibacterial activity. Most of the compounds exhibited significant antifungal and antibacterial activity against all the tested strains.
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