期刊
MARINE DRUGS
卷 10, 期 8, 页码 1711-1728出版社
MDPI AG
DOI: 10.3390/md10081711
关键词
pseudopteroxazoles; semi-synthesis; Mycobacterium tuberculosis; antibiotic-resistance
资金
- Natural Sciences and Engineering Council of Canada (NSERC)
- Canada Research Chair Program
- Atlantic Innovation Fund
- Jeanne and Jean-Louis Levesque Foundation
- National Research Council's Industrial Research Assistance Program (IRAP)
Pseudopterosins and pseudopteroxazole are intriguing marine natural products that possess notable antimicrobial activity with a commensurate lack of cytotoxicity. New semi-synthetic pseudopteroxazoles, pseudopteroquinoxalines and pseudopterosin congeners along with simple synthetic mimics of the terpene skeleton were synthesized. In order to build structure-activity relationships, a set of 29 new and previously reported compounds was assessed for in vitro antimicrobial and cytotoxic activities. A number of congeners exhibited antimicrobial activity against a range of Gram-positive bacteria including Mycobacterium tuberculosis H(37)Rv, with four displaying notable antitubercular activity against both replicating and non-replicating persistent forms of M. tuberculosis. One new semi-synthetic compound, 21-((1H-imidazol-5-yl)methyl)-pseudopteroxazole (7a), was more potent than the natural products pseudopterosin and pseudopteroxazole and exhibited equipotent activity against both replicating and non-replicating persistent forms of M. tuberculosis with a near absence of in vitro cytotoxicity. Pseudopteroxazole also exhibited activity against strains of M. tuberculosis H(37)Rv resistant to six clinically used antibiotics.
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