| Literature DB >> 27657808 |
Bahubali M Chougala1, S Samundeeswari1, Megharaja Holiyachi1, Lokesh A Shastri2, Suneel Dodamani3, Sunil Jalalpure4, Sheshagiri R Dixit5, Shrinivas D Joshi5, Vinay A Sunagar6.
Abstract
A green, eco-friendly and efficient protocol has been developed and synthesized a series of coumarin based pyrano[2,3-c]pyrazole derivatives (3) by multi-component reaction (MCR). Unexpected 3-coumarinyl-3-pyrazolylpropanoic acids (4) have been isolated by the reaction of compound (3) in acidic conditions. Further, intramolecular cyclization of compounds (4) leads to C4C4 chromons (9) and these compounds were screened for their biological activities using array of techniques. Most of the compounds exhibited promising antibacterial activity, in particular Gram-positive bacteria. The anti-inflammatory assay was evaluated against protein denaturation as well as HRBC membrane stabilization methods and compounds exhibit excellent anti-inflammatory activity in both methods. Molecular docking study has been performed for all the synthesized compounds with S. aureus dihydropteroate synthetase (DHPS) and results obtained are quite promising. Copyright ÂEntities:
Keywords: 3-Coumarinyl-3-pyrazolylpropanoic acids; Anti-inflammatory; Antibacterial; C(4)C(4) pyranone; DMAP; Molecular docking; Pyrano[2,3-c]pyrazole; Pyranopyrazolo-pyrimidine
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Year: 2016 PMID: 27657808 DOI: 10.1016/j.ejmech.2016.09.021
Source DB: PubMed Journal: Eur J Med Chem ISSN: 0223-5234 Impact factor: 6.514