Application of clinafloxacin amino derivatives and medicinal salts thereof in preparing antitubercular medicaments

A technology of derivatives and star amino, which is applied to compounds in the fields of pharmacy and chemistry, and can solve unclear problems
CN103405435BActive Publication Date: 2014-12-10SOUTHWEST UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SOUTHWEST UNIV
Publication Date
2014-12-10

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Abstract

The invention discloses an application of clinafloxacin amino derivatives and medicinal salts thereof in preparing antitubercular medicaments. In the structural general formula of the clinafloxacin amino derivatives, R is -(CH2)nNR<1>R<2>, -CH(CH2CH2XCH3)NH2, 2-pyrrolidyl or -OR3; n is 0 or 1; R1 and R2 are separately hydrogen, methyl, 2-hydroxyethyl, (R)-1-ethyl-2-hydroxyethyl, 2-aminoethyl, 3-(dimethylamino)propyl, hydroxyl, amino, methylamino, methoxyl or thiourea group; X is S or SO2; R3 is methyl or isobutyl; the compounds have certain inhibitory effect on standard sensitive strains, clinically isolated sensitive strains and clinically isolated drug-resistant strains of mycobacterium tuberculosis, the antitubercular activity of a part of compounds is stronger than that of ofloxacin and clinafloxacin and weaker than that of moxifloxacin, thus providing a new research direction for the antitubercular medicaments, and being beneficial to clinical treatment of tuberculosis.
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Description

Technical field

[0001] The invention belongs to the field of chemistry and relates to new uses of compounds in the field of pharmacy. Background technique

[0002] Tuberculosis caused by mycobacteria is a highly infectious chronic disease, and its population infection rate has remained high since ancient times. my country is one of the 22 countries with a high burden of tuberculosis in the world, and the number of patients is second only to India. There are many reasons for the rebound of the tuberculosis epidemic in some areas. There are objective reasons such as the rapid increase in the floating population, the spread of drug-resistant tuberculosis, and the dual infection of tuberculosis and HIV. More importantly, the general lack of attention to tuberculosis health education. Knowledge of tuberculosis prevention and treatment is not popularized. At present, the first-line treatment drugs for common tuberculosis, such as rifampicin (RFP), isoniazid (INH), pyrazinamide (PZA),...

Claims

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