Add time:07/12/2019         Source:sciencedirect.com

A series of novel 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives were synthesized and evaluated for anti-hepatitis B virus (anti-HBV) activities in vitro to explore their structure–activity relationships (SARs). Most of the synthesized compounds possessed potent anti-HBV activity, of which the promising compound 44 exhibited significantly inhibitory potency against the secretion of hepatitis surface antigen (HBsAg) (IC50 = 0.010 mM, SI > 135), hepatitis e antigen (HBeAg) (IC50 = 0.026 mM, SI > 51) and the replication of HBV DNA (IC50 = 0.045 mM). Preliminary mechanism study suggested compound 44 could mainly enhance the transcript activity of HBV ENI (enhancer I), EN-II (enhancer II).

► We synthesized a series of new non-nucleoside 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one analogues via chemical modifications on N-1, C-2, and hydroxyethyl moiety. ► These analogues were further evaluated their anti-HBV activities to explore their structure-activity relationships. ► Preliminary mechanism study suggested the promising compound 44 could mainly enhance the transcript activity of HBV ENI (enhancer I), ENII (enhancer II).

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