Use of compound scalarafuran

A compound and application technology, applied in the fields of medicinal chemistry and pharmacotherapeutics, can solve problems such as the uncertainty of whether the compound has a direct effect, the toxic and side effects of HIV drug-resistant reverse transcriptase and protease inhibitors, and the lack of drugs for IN inhibitors.
CN1864691AInactive Publication Date: 2006-11-22SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Publication Date
2006-11-22
Estimated Expiration
Not applicable · inactive patent

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Abstract

The present invention discloses one kind of compound, citiofuran. The compound, citiofuran has very high combination activity, KD=16.4 microM, with HIV-1 integrase, and effective inhibition of the combination of the integrase to the substrate, IC50=120 microM, in substrate competition test. Therefore, the compound exhibits very high medicine preparing value.
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Description

technical field

[0001] The invention relates to the fields of medicinal chemistry and pharmacotherapeutics, in particular to a preparation method and application of a sesquiterpene compound scalarafuran. Background technique

[0002] Since the first AIDS (acquired immunodeficiency syndrome) patient was discovered in the United States in 1981, AIDS has spread rapidly in more than 180 countries and regions around the world. At present, the total number of AIDS patients and virus carriers in the world has reached more than 42 million, of which nearly 1 million are in China, ranking second in Asia and 14th in the world. Moreover, in recent years, the number of AIDS cases in China has been increasing rapidly at an average annual rate of 30-40%, which has become an increasingly serious public security problem.

[0003] As the pathogen of AIDS, HIV virus needs the participation of integrase (IN) to complete the replication process in the body after it infects the human body. IN c...

Claims

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