Synthesis of azaisoflavones and their inhibitory activities of NO production in activated microglia.
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 microM 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.
College of Pharmacy, Sookmyung Women's University, 52 Hyochangwon-Gil, Yongsan-Gu, Seoul 140-742, Republic of Korea.
Guo Hua
GH
Jin
Sang Keun
SK
Ha
Hye Min
HM
Park
Bomi
B
Kang
Sun Yeou
SY
Kim
Hee-Do
HD
Kim
Jae-Ha
JH
Ryu
Raok
R
Jeon
D000818:Animals; D002460:Cell Line; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D020128:Inhibitory Concentration 50; D007529:Isoflavones / Q000737:chemistry*; D051379:Mice; D017628:Microglia / Q000187:drug effects / Q000378:metabolism*; D008956:Models, Chemical; D009569:Nitric Oxide / Q000737:chemistry*; D052247:Nitric Oxide Synthase Type II / Q000378:metabolism*; D015363:Quinolones / Q000737:chemistry; D013696:Temperature; D013778:Tetrazolium Salts / Q000494:pharmacology; D013844:Thiazoles / Q000494:pharmacology
D007529:Isoflavones; D015363:Quinolones; D013778:Tetrazolium Salts; D013844:Thiazoles; D009569:Nitric Oxide; D052247:Nitric Oxide Synthase Type II; C022616:thiazolyl blue