This research is focused on designing, synthesis and biological evaluation of a series of coumarin based benzothiazole derivatives. The ligands were identified by docking study for antioxidant and antibacterial potential using target proteins PDB:4H1J and PDB:3G75, respectively. The target molecules were synthesized as a series of substituted N-(benzothiazol-2-yl)-2-oxo-chromene-3-carboxamides (7a–h) by condensation of substituted benzo[d]thiazol-2-amines with in situ synthesized substituted 2-oxo-2H-chromene-3-carbonyl chlorides. Infrared spectroscopy and 1 H- nuclear magnetic resonance spectra were used to characterize the synthesized molecules. In vitro antioxidant activity of compounds was evaluated by DPPH and H2 O2 radical scavenging assays. Antibacterial potential of compounds was evaluated using well diffusion method against Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922) and Pseudomonas aeruginosa (ATCC 27853). Among synthesized derivatives, 7a showed good antioxidant potential whereas 7f showed antibacterial activity, which might be employed as lead molecules for future investigation for respective activities.
Euphorbia fusiformis Buch.-Ham.Ex D.Don, (Synonym: Euphorbia acaulis Roxb) is an infrequent medicinal, geophytic herb belonging to family Euphorbiaceae. The latex obtained from tubers of Euphorbia fusiformis was traditionally used as an antidote in scorpion and snake bites. Fresh latex has been externally applied to heal chronic wounds and cracks and to cure skin diseases. Previous research on the Euphorbia fusifornis primarily focused on phytochemical investigation and pharmacological screening of various solvent extracts of dried root powder. Considering the therapeutic potential of the latex, there is a need to explore the studies on plant latex. The present work deals with the determination of physicochemical properties, preliminary phytochemical analysis and acute oral toxicity study of latex of Euphorbia fusiformis. Physicochemical characterization and preliminary phytochemical studies were carried out by using ethanolic solution of latex. The studies revealed the presence of alkaloids, glycosides, terpenoids, steroids and saponins. Acute oral toxicity study of latex were carried out by acute toxic class method of OECD 423 guideline. Euphorbia fusiformis latex was found to be safe at the dose of 2000 mg/kg and therefore characterized as Category 5 in the GHS system. It is concluded that further studies are essential for isolation and identification of chemical constituents from Euphorbia fusiformis and screening of pharmacological activities to support the traditional claims.
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