4.3 Article

Design, synthesis, characterization, and biological evaluation of pyrido[1,2-a]pyrimidinone coumarins as promising anti-inflammatory agents

Journal

SYNTHETIC COMMUNICATIONS
Volume 48, Issue 4, Pages 375-386

Publisher

TAYLOR & FRANCIS INC
DOI: 10.1080/00397911.2017.1397698

Keywords

2-Aminopyridine; 4-formaylcoumarin; Baylis Hillman adducts; cyclocondensation; environmentally friendly; fused pyridopyrimidinones

Funding

  1. Rajiv Gandhi National Fellowship [F1-17.1/2015-16/RGNF-2015-17-SC-KAR-3771/(SA-III/W)]

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Pursuing our recent interest regarding antimicrobial and anti-inflammatory activities of coumarin derivatives, we have synthesized a series of coumarin-linked pyridopyrimidinones by using Baylis Hillman adduct in aqueous condition with high purity. Pyrido[1,2-a]pyrimidin-2-ones are important class of heterocyclic compounds because of their use in medicinal and agro chemistry as active agents. All these newly synthesized compounds were evaluated for their antimicrobial and anti-inflammatory activity. Coumarin pyridopyrimidinones showed excellent anti-inflammatory activity against both MMP-2 and MMP-9 gelatinase zymography, whereas considerable good activity against Gram-positive and Gram-negative bacterial strains; however, antifungal activity observed in these series is more or less inactive. The active compounds of these series would be promising structural templates for the development of novel and more efficient anti-inflammatory agent.

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