Oroxylin A analogs exhibited strong inhibitory activities against iNOS-mediated nitric oxide (NO) production

A number of oroxylin A analogs were prepared and evaluated for their inhibitory activities against iNOS-mediated nitric oxide (NO) production from LPS-stimulated BV2 cells. The analogs were synthesized from purchased 2′-hydroxy-4,5,6-trimethoxyacetophenone and aldehydes in 3 steps. Among the tested...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-04, Vol.22 (7), p.2534-2535
Hauptverfasser:	Pham, Tuan-Ahn. N., Che, Haiyan, Phan, Phuong-Thuy T., Lee, Jae-Won, Kim, Sung-Soo, Park, Haeil
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetophenones - chemistry Aldehydes Aldehydes - chemistry Animals Anti-Anxiety Agents - chemical synthesis Anti-Anxiety Agents - pharmacology Anti-inflammatory activity Biological and medical sciences Cell Line, Transformed Flavanones - pharmacology Flavonoids - chemical synthesis Flavonoids - pharmacology inducible nitric oxide synthase Inhibition of NO production Lipopolysaccharides - pharmacology Macrophages - cytology Macrophages - drug effects Medical sciences Mice Microglia - cytology Microglia - drug effects Nitric oxide Nitric Oxide - antagonists & inhibitors Nitric Oxide - biosynthesis Nitric Oxide Synthase Type II - antagonists & inhibitors Nitric Oxide Synthase Type II - metabolism Nitrophenols - chemistry Oroxylin A and its analogs Pharmacology. Drug treatments Wogonin
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Zusammenfassung:	A number of oroxylin A analogs were prepared and evaluated for their inhibitory activities against iNOS-mediated nitric oxide (NO) production from LPS-stimulated BV2 cells. The analogs were synthesized from purchased 2′-hydroxy-4,5,6-trimethoxyacetophenone and aldehydes in 3 steps. Among the tested compounds, several analogs (3b, 3c, 3d, 3f) exhibited strong inhibitory activities. Especially, the analog with 4-nitrophenyl group (3b) showed stronger inhibitory activity (IC50=4.73μM) than that of wogonin (IC50=7.80μM). A number of oroxylin A analogs were prepared and evaluated for their inhibitory activities against iNOS-mediated nitric oxide (NO) production from LPS-stimulated BV2 cells. The analogs were synthesized from purchased 2′-hydroxy-4,5,6-trimethoxyacetophenone and aldehydes in 3 steps. Among the tested compounds, several analogs (3b, 3c, 3d, 3f) exhibited strong inhibitory activities. Especially, the analog with 4-nitrophenyl group (3b) showed stronger inhibitory activity (IC50=4.73μM) than that of wogonin (IC50=7.80μM).
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2012.01.135