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Novel Pyridazino[4,3-b]indoles with Dual Inhibitory Activity against Mycobacterium tuberculosis and Monoamine Oxidaseстатья Исследовательская статья
Статья опубликована в высокорейтинговом журнале
Статья опубликована в журнале из списка Web of Science и/или Scopus- Авторы: Velezheva Valeriya S., Brennan Patrick J., Marshakov Vladimir Yu, Gusev Dmitrij V., Lisichkina Inessa N., Peregudov Alexander S., Tchernousova Larisa N., Smirnova Tatiana G., Andreevskaya Sofia N., Medvedev Alexei E.
- Журнал: Journal of Medicinal Chemistry
- Том: 47
- Номер: 13
- Год издания: 2004
- Издательство: American Chemical Society
- Местоположение издательства: United States
- Первая страница: 3455
- Последняя страница: 3461
- DOI: 10.1021/jm030479g
- Аннотация: Tuberculosis is one of the most common infectious diseases known to man. About 37% of the world's population (about 1.86 billion people) are infected with Mycobacterium tuberculosis. According to the World Health Organization, every year approximately 8 million people develop active tuberculosis and almost 2 million of those die from the disease. The incidence of multidrug-resistant tuberculosis (MDR-TB) is increasing. The present drug regimen for treating tuberculosis has been in existence for 30 years. New drugs that will shorten total treatment duration, improve the treatment of MDR-TB, and address latent tuberculosis are the most urgent need of tuberculosis control programs. A new series of synthetic 3-amino-4-arylpyridazino[4,3-b]indoles (pyridazinoindoles) were identified as inhibitors of Mycobacterium tuberculosis. The design, synthesis, and antimycobacterial activity of these compounds are described. While the most active compounds are still not comparable to the front-line drugs rifampicin and isoniazid, they do show promise. Most of the pyridazinoindoles with appreciable antituberculosis activity also inhibit monoamine oxidase, suggestive of a novel inhibitory effect on mycobacterial redox reactions.
- Добавил в систему: Алексеева Екатерина Александровна