کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1355066 | 1500447 | 2016 | 9 صفحه PDF | دانلود رایگان |
• 7-Subsituted coumarin derivatives were design, synthesize and characterized.
• Compounds showed interactions with the key amino acid residues of 5-LOX enzyme.
• Compounds 33 and 35 showed anti-inflammatory, analgesic and LOX inhibitory activity.
• Compound 35 showed mixed or non-competitive type of inhibition with 5-LOX enzyme.
In the present study, 7-subsituted coumarin derivatives were synthesized using various aromatic and heterocyclic amines, and evaluated in vivo for anti-inflammatory and analgesic activity, and for ulcerogenic risk. The most active compounds were evaluated in vitro for 5-lipoxygenase (5-LOX) inhibition. Docking study was performed to predict the binding affinity, and orientation at the active site of the enzyme. In vivo anti-inflammatory and analgesic activity, and in vitro 5-LOX enzyme inhibition study revealed that compound 33 and 35 are the most potent compounds in all the screening methods. In vitro kinetic study of 35 showed mixed or non-competitive type of inhibition with 5-LOX enzyme. Presence of OCH3 group in 35 and Cl in 33 at C6-position of benzothiazole ring were found very important substitutions for potent activity.
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Journal: Bioorganic Chemistry - Volume 67, August 2016, Pages 130–138