Abstract:
: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.
journal_name
Bioorg Chemjournal_title
Bioorganic chemistryauthors
Srivastava P,Vyas VK,Variya B,Patel P,Qureshi G,Ghate Mdoi
10.1016/j.bioorg.2016.06.004subject
Has Abstractpub_date
2016-08-01 00:00:00pages
130-8eissn
0045-2068issn
1090-2120pii
S0045-2068(16)30083-9journal_volume
67pub_type
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