Quinoline-based compounds are one of the most important classes of N-heterocyclics exhibiting a wide spectrum of biological activities. There is a constant demand for the synthesis of new quinoline-based molecules suitable for therapeutic applications. Here a new strategy is developed to synthesize different quinoline-based quinazolinones catalytically using InCl 3 through a cyclocondensation reaction of isatoic anhydride and aniline with 2-substituted-quinoline-3-carbaldehyde to produce 2-(2-phenoxyquinolin-3-yl)-3-phenyl-2,3-dihydroquinazolin-4(1H)-one derivatives (> 90 % yields). In contrast, the reduced electrophilicity at the metal center allows the hydrazide ligand to bind In(III) and serendipitously forms benzoic(2-phenoxyquinoline-3-carbonyl) carbamic anhydride (∼ 70 % yields). The mechanistic aspects of these reactions were rationally explained. The structure and purity of all the isolated derivatives were assessed by spectroscopic and analytical data. In view of a strong correlation existing between inflammation and cancer progression, the ex-vivo anti-inflammatory effect of the ligands was established. The anti-cancer property of the proposed ligand was delineated with a specific SIRT protein family. Further, the computational docking studies on the binding abilities of 22 synthesized compounds with the Sirt1 protein were discussed in detail.
In wound care there is room for delivering antibiotic drug at wound site to avoid or control the infections. This current work is about preparation and evaluation of poly(lactic-co-glycolic acid) (PLGA) and poly(caprolactone) (PCL) based, gentamicin (GE) loaded biodegradable material to get optimum drug at site for antibacterial action. Drug release, degradation behaviour and tensile properties of prepared bio-material are studied up to 42 days. Drug release in in-vitro release testing (IVRT) was studied by UV absorbance of receptor solution. Physical characteristics such as molecular weight, tensile strength and morphology of bio-material are carried out as a function of time during IVRT studies. The employed bio-material releases 3.4 μg/g/h drug with a steady decrease in tensile strength and PLGA molecular weight. In this manuscript it is demonstrate that PLGA and PCL based bio-material will release the loaded drug in controlled manner with simultaneous degradation.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.