RESUMO
Objective: To study physicochemical properties, antioxidant and anti-inflammatory activities of coumarin-carbonodithioate hybrids. Methods: The substituted 4-bromomethyl coumarins were synthesized in first step by the cyclization. Then the reaction of substituted coumarins (a-e) with potassium O-ethyl/methyl carbonodithioate (1) by using absolute ethanol as solvent,afforded coumarin-carbonodithioate (1a-1j) derivatives under microwave irradiation and the conventional method. The spectroscopic analysis was used for the characterization of coumarin derivatives. The title (1a-1j) compounds were confirmed by spectroscopic methods.Antioxidant property was evaluated by using DPPH free radical-scavenging ability assay method and anti-inflammatory activity was evaluated by protein denaturation procedure using diclofenac sodium as a standard. Drug-likeness. In-silico toxicity was predicted with LD50 value and bioactivity score was also calculated for all the compounds. Results: All coumarin (1a-1j) compounds exhibited promising in-vitro antioxidant and anti-inflammatory properties in comparison to standard drugs. All tested compounds were used for evaluating their physicochemical properties as set by Lipinski rule. It was observed that the synthesized compounds followed rule of five, indicating more 'drug-like' nature. Conclusions: All the screened coumarin-carbonodithioates display promising in vitro antioxidant and antiinflammatory activities. From the physicochemical properties of coumarin derivatives, it is found that none of the compounds violate the Lipinski rule and they fall well in the range of rule of five. It is concluded that the coumarin-carbonodithioate hybrids act with more 'drug-like' nature.
RESUMO
Objective: To study physicochemical properties, antioxidant and anti-inflammatory activities of coumarin-carbonodithioate hybrids. Methods: The substituted 4-bromomethyl coumarins were synthesized in first step by the cyclization. Then the reaction of substituted coumarins (a-e) with potassium O-ethyl/methyl carbonodithioate (1) by using absolute ethanol as solvent, afforded coumarin-carbonodithioate (1a-1j) derivatives under microwave irradiation and the conventional method. The spectroscopic analysis was used for the characterization of coumarin derivatives. The title (1a-1j) compounds were confirmed by spectroscopic methods. Antioxidant property was evaluated by using DPPH free radical-scavenging ability assay method and anti-inflammatory activity was evaluated by protein denaturation procedure using diclofenac sodium as a standard. Drug-likeness. In-silico toxicity was predicted with LD
RESUMO
Aims: The present work was decided to evaluate the in-vitro anti-inflammatory activity of crude extracts of Bombax ceiba in order to characterize the role of this extract in affecting the inflammatory process. Study Design: Extraction of B. ceiba bark, phytochemical screening, and evaluation of invitro anti-inflammatory activity. Methodology: Petroleum ether, ethanol and aqueous extracts of B. ceiba barks were prepared by maceration technique and subjected to preliminary phytochemical tests. The in-vitro anti-inflammatory activity of all extracts (1000 mcg/ml) was assessed by HRBC membrane stabilization method. Results: Ethanol extract showed significant (p<0.001) response followed by aqueous extract (p<0.01) when compared with standard, diclofenac potassium (50 mcg/ml). Conclusion: The study suggests that the extracts possess enough potential to reduce inflammation by in-vitro and directs the importance of further research and development of novel anti-inflammatory agents.