Medical use of compound hyrtiosal

The technology of a compound, aldehyde, is applied in the field of medicinal chemistry and pharmacotherapeutics, which can solve problems such as unclear mechanism, false positive, and uncertainty about whether the compound has a direct effect.
CN1864674BInactive Publication Date: 2010-04-14SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Publication Date
2010-04-14
Estimated Expiration
Not applicable · inactive patent

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Abstract

The present invention discloses one kind of compound, citioaldehyde. The compound, citioaldehyde has very high combination activity, KD=0.197 microM, with HIV-1 integrase, and effective inhibition ofthe combination of the integrase to the substrate, IC50=9.6 microM, in substrate competition test. Therefore, the compound will find its application in preventing and treating AIDS.
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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 of a sesquiterpene compound hyrtiosal and research on HIV-1 integrase inhibitory activity. 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...

Claims

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