N-phenyl-4-phenylbutyramide oxime and its derivatives with anti-hepatitis B virus activity

Abstract

The invention discloses N-phenyl-4-phenyl butyrylamide oxime with anti-hepatitis B virus activity and a derivative thereof. The structure of the N-phenyl-4-phenyl butyrylamide oxime is represented by the following general formula: shown in the specification. An in-vitro HepG2.2.15 cell activity experiment shows that the N-phenyl-4-phenyl butyrylamide oxime has a certain inhibition effect on HBV surface antigens (HBsAg) and e antigens (HBeAg). Under the same condition, the inhibition rates of positive reference drug Lamivudine to HBsAg and HBeAg are respectively 50.9 percent and 45.2 percent, while the compound disclosed by the invention has the inhibition rates to HBsAg and HBeAg of 91.7 percent and 59.5 percent. The structure of the novel N-phenyl-4-phenyl butyrylamide oxime is different from that of a nucleoside similar drug, so that the N-phenyl-4-phenyl butyrylamide oxime is obvious in inhibition to the HBV activity, low in toxicity and expected to be further developed into a novel anti-hepatitis B virus drug.

Description

technical field

[0001] The invention belongs to N-benzamide-oxime compounds, in particular to N-phenyl-4-phenylbutyramide oxime and its derivatives with anti-hepatitis B virus activity. Background technique

[0002] Viral hepatitis type B (viral hepatitis type B), referred to as hepatitis B, is a common infectious disease caused by hepatitis B virus (Hepatitis B virus, HBV). advanced features. Hepatitis B is a serious global health problem that causes chronic liver disease and infection, and its patients are at high risk of dying from cirrhosis and liver cancer. About 1 / 2 of the world's population lives in HBV-susceptible areas, about 2 billion people have been proven to have been infected with HBV, 300-400 million people are chronically infected with HBV, and about 780,000 people die of acute or chronic hepatitis B every year. The etiology ranks 10th. China is the country with the largest number of people infected with hepatitis B virus in the world. About 690 million pe...

Images