Abstract
A series of 4-aryl-2,6-dimethyl-3,5-bis-N-(aryl)-carbamoyl-1,4-dihydropyri-dines 6a-6h were prepared by using the one-pot three component synthetic method. The target compounds 6a-6h were synthesized by reacting two molar equivalents of ketone functionality and one mole of aromatic aldehydes in ammonium acetate to obtain the desired products. The structures of newly synthesized compounds were characterized by FT-IR, 1H-NMR, 13C-NMR, and elemental analysis. All the synthesized compounds were screened for their elastase inhibition and antioxidant activity. Almost all of the com-pounds 6a-h showed good to excellent activities against elastase enzyme more than the reference drug. Compounds 6d and 6b at 0.2 ± 0.0 µM and 0.2 ± 0.0 µM were found to most potent derivatives against elastase enzyme. Compound 6a exhibited prominent free radical scavenging activity. From the results of the biological activity, we infer that some derivatives can serve as lead molecules in pharmacology.
 Video Clip of Methodology:
 3 min 13 sec Full Screen Alternate
Highlights
The dazzling and fresh appearance of skin does not last for very long
The physiological damage to the skin can be either extrinsic or intrinsic and storage of reactive oxygen species (ROS) in human skin can lead to activation of skin disease causing enzymes such as tyrosinase and elastase enzymes (Popoola et al, 2015)
Elastase enzyme degrades the elastin, inhibition of elastase activity can serve as an efficient way to protect skin aging
Summary
The physiological changes in the skin are inevitable and dermatologists are keenly involved in exploring the potent inhibitors for skin protection. The physiological damage to the skin can be either extrinsic or intrinsic and storage of reactive oxygen species (ROS) in human skin can lead to activation of skin disease causing enzymes such as tyrosinase and elastase enzymes (Popoola et al, 2015). Elastase is an enzyme which belongs to the family of chymotrypsin and it is responsible for the cleavage of elastin (Macdonald et al, 1998). Elastin is a protein present in the skin and is responsible for the skin elasticity. Elastin forms the elastic fiber which furnishes elasticity to connective tissues. Elastase enzyme degrades the elastin, inhibition of elastase activity can serve as an efficient way to protect skin aging
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
