1441772-25-3Relevant articles and documents
Synthesis and biological evaluation of novel 2′,4′,5′- trimethoxyflavonol derivatives as anti-inflammatory and antimicrobial agents
Hatnapure, Girish D.,Keche, Ashish P.,Rodge, Atish H.,Tale, Rajesh H.,Birajdar, Satish S.,Pawar, Mahendra J.,Kamble, Vandana M.
, p. 461 - 470 (2014/03/21)
A series of novel 3-hydroxy-2-(2,4,5-trimethoxyphenyl)-4H-chromen-4-one (flavonol) derivatives (2a-u) of biological interest have been prepared via CLAISEN-SCHMIDT condensation followed by ALGAR-FLYNN-OYAMADA reaction and to search for the potent nonsteroidal anti-inflammatory agents from this novel series. All the synthesized compounds have been screened for their in vitro proinflammatory cytokines tumor necrosis factor (TNF-α) and interleukin-6 (IL-6) inhibitory activity along with antimicrobial activity. As many as three compounds viz. 2h, 2l, and 2q from this novel series were found to be potent TNF-α and IL-6 inhibitor (up to 72-81 % TNF-α and 86-92 % IL-6 inhibitory activity) but at 10 μM concentration as compared with the standard dexamethasone (71 % TNF-α and 84 % IL-6 inhibitory activities at 1 μM concentration). While the compounds 2d, 2m, 2n, and 2s were found to be potent antimicrobial agent showing even 2-2.5-fold more potency than that of standard ciprofloxacin and miconazole at the same MIC value of 10 μg/mL.
