Preparation method and use of novel S-DABO HIV-1 reverse transcriptase inhibitor

A technology of HIV-1 and reagents, applied in the medical field, can solve problems such as drug-resistant strains
CN101597263AInactive Publication Date: 2009-12-09CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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Patent Information

Authority / Receiving Office
CN Β· China
Patent Type
Applications(China)
Current Assignee / Owner
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
Publication Date
2009-12-09
Estimated Expiration
Not applicable Β· inactive patent

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Abstract

The invention relates to a novel S-DABO compound which is designed by taking non-nucleoside HIV-1 reverse transcriptase inhibitor 3,4- dihydro-2-alkoxy-6-benzyl-4- carbonyl pyrimidine (DABO) and 1-[(2- hydroxy ethoxy) methyl]-6- thiophenyl thymine (HEPT) as lead compounds, combining research results of the research team, connecting and merging each structure and activity relationship in a molecule according to a basic principle of reasonable drug design. The novel S-DABO compound is shown in the general formula I, and definition of each group is disclosed as description in an affidavit of claim. In the invention, the C2, C4 and C5 sites of a pyrimidine ring are modified through various different groups to obtain the novel compound which is more beneficial to be combined with HIV-1 reverse transcriptase with the structure. Through HIV RT activity test, the novel S-DABO HIV-1 reverse transcriptase inhibitor has higher activity, wherein the activity of one compound is higher than 23 times of nevirapine currently used in clinic; and the compound can become a novel class of latent drug for resisting AIDS.
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Description

technical field

[0001] The application relates to non-nucleoside HIV-1 (human immunodeficiency virus-1) reverse transcriptase inhibitor 3,4-dihydro-2-alkoxy-6-benzyluracil (DABO) and 1-[ (2-Hydroxyethoxy)methyl]-6-phenylthiothymine (HEPT) is used as a lead substance, and with reference to the substrate conformation of HIV-1 reverse transcriptase (HIV-1RT) that acts on this type of compound, design, A series of novel S-DABO compounds were synthesized and tested for their biological activity. Non-nucleoside HIV-1 type reverse transcriptase inhibitors have been developed into more than 30 compounds with different structures, among which three compounds, nevirapine, delavirdine and efavirenz, have been For clinical use, there are also a variety of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in clinical trials. Among them, DABO compounds have become an important class of non-nucleoside HIV-1 reverse transcriptase inhibitors since they were first discovered in 1992. T...

Claims

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