SYNTHESIS, CHARACTERIZATION AND ANTI INFLAMMATORY ACTIVITY OF NOVEL QUINOXALINE DERIVED CHALCONES
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2015, Vol 7, Issue 1
Abstract
Objective: Quinoxaline derivatives were reported with wide range of biological activities. Hence it was planned to synthesize and screen for their anti inflammatory (in vivo) activity.Methods: Orthophenylene diamine was reacted with oxalic acid to form quinoxaline 2, 3 dione. Quinoxaline-2, 3 (1H, 4H)-dione was chlorinated by using Phosphorousoxytrichloride (POCl3) in dimethyl formamide, to form 2, 3- dichloroquinoxaline. This dichloride compound was reacted with 4 amino acetophenone in DMF, refluxed for 5 hours to form 1-(4-(3-chloroquinoxalin-2-ylamino) phenyl) ethanone. Similarly 1-(4-(3-chloroquinoxalin-2-ylamino) phenyl) ethanone was reacted with corresponding aromatic aldehydes to form quinoxaline derived chalcone by Claisen Schmidt reaction. Characterization all the compounds was performed by IR, 1H NMR and Mass spectroscopic data and screened for anti- inflammatory activity by carrageenan- induced paw edema method.Results: The anti inflammatory data suggested that compounds QCAC 2, 6, 8, 9, 10 and 12 showed significant activity and rest of the compounds exhibited moderate activity compared to the standard compoundConclusion: The compounds bearing nitro, chloro and methoxy groups have shown prominent activity when compared to compounds without these groups.Â
Authors and Affiliations
Karakavalasa Pradeep, Vijay Kotra, R. L Priyadarshini, Veeresh Pratap
EXTRACTION AND ISOLATION OF FLAVONOID QUERCETIN FROM THE LEAVES OF TRIGONELLA FOENUM-GRAECUM AND THEIR ANTI-OXIDANT ACTIVITY
Objective: The present study was designed for isolation of bioactive flavonoid molecule quercetin from the leaves of Trigonella foenum-graecum and their subsequent characterization. Methods: Crude extracts of fenugreek w...
SCREENING AND ANTIBIOGRAM PATTERN OF BACTERIAL OPHTHALMIC INFECTIONS
Objective: Microbial infections are causing life threatening diseases of which ocular infection is of primary importance, as it can even led to blindness. In order to understand the etiological agents causing bacterial o...
PHYSICO-MECHANICAL AND FILM-FORMING PROPERTIES OF CARBOXYMETHYL CORN STARCH BUTYRATE
Objective: This study aims to prepare a new hydrophobic, water-soluble modified corn starch via sequential butyrylation and carboxymethylation and to evaluate its physico-mechanical and film-forming properties.Methods: B...
FORMULATION, DEVELOPMENT AND IN VITRO EVALUATION OF TRAMADOL EXTENDED RELEASE TABLETS
Objective: The objective of the present study was to develop “once daily” extended release tablets of tramadol (100 mg) by wet granulation using hydrophilic polymer like hydroxy propyl methyl cellulose K100M,K15M and pol...
ORAL GENTAMICIN PREPARATION USING SOLIDIFIED LIPID PARTICULATE DELIVERY SYSTEM
Objective: Despite the broad pharmacological activity of gentamicin against a number of bacteria, it's very inadequate oral bioavailability due to poor intestinal membrane permeability has limited its formulation into or...