Synthesis of azaisoflavones and their inhibitory activities of NO production in activated microglia

• Published in: Bioorganic & medicinal chemistry Vol. 18; no. 14; pp. 4092 - 4094
• Main Authors: Jin, Guo Hua, Ha, Sang Keun, Park, Hye Min, Kang, Bomi, Kim, Sun Yeou, Kim, Hee-Do, Ryu, Jae-Ha, Jeon, Raok
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 15.07.2008; Elsevier
• Subjects: Animals; Azaisoflavone; Biological and medical sciences; Cell Line; Chemistry, Pharmaceutical - methods; Drug Design; Inhibitory Concentration 50; iNOS; Isoflavones - chemistry; Medical sciences; Mice; Microglia - drug effects; Microglia - metabolism; Miscellaneous; Models, Chemical; Neuropharmacology; Nitric oxide; Nitric Oxide - chemistry; Nitric Oxide Synthase Type II - metabolism; Pharmacology. Drug treatments; Quinolones - chemistry; Temperature; Tetrazolium Salts - pharmacology; Thiazoles - pharmacology; Azaisoflavone; iNOS; Nitric oxide; Azaisoflavone,Nitric oxide,iNOS; Enzyme; Isozyme; Rodentia; Quinoline derivatives; In vitro; Biological activity; Nitric-oxide synthase; Microglia; Vertebrata; Mammalia; Cell line; Mouse; Production; Phenols; Oxidoreductases; Inhibition; Chemical synthesis; Quinolone derivatives
• ISSN: 0960-894X; 0968-0896; 1464-3405; 1464-3391
• DOI: 10.1016/j.bmcl.2008.05.106

Synthesis of series of azaisoflavones and their inhibitory activities on the NO production in lipopolysaccharide activated micoglia are reported. A series of azaisoflavones were synthesized and their biological activities were evaluated for nitric oxide (NO) production and inducible NO synthase (iNOS) expression in BV-2 microglia cell lines. Among these compounds, compound 8d was the most potent with IC 50 7.83 μM for inhibition of NO production. Also, compound 8d inhibited expression of iNOS in LPS-induced BV2 cells. This result suggests that compound 8d inhibited the production of NO by suppressing the expression of iNOS.