Evaluation of Pseudopteroxazole and Pseudopterosin Derivatives against Mycobacterium tuberculosis and Other PathogensReportar como inadecuado




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1

Department of Chemistry and Department of Biomedical Sciences, Atlantic Veterinary College, University of Prince Edward Island, Charlottetown, PEI C1A 4P3, Canada

2

Nautilus Biosciences Canada, Inc., Charlottetown, PEI C1A 4P3, Canada





*

Author to whom correspondence should be addressed.



Abstract 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 H37Rv, 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-ylmethyl-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 H37Rv resistant to six clinically used antibiotics. View Full-Text

Keywords: pseudopteroxazoles; semi-synthesis; Mycobacterium tuberculosis; antibiotic-resistance pseudopteroxazoles; semi-synthesis; Mycobacterium tuberculosis; antibiotic-resistance





Autor: Malcolm W. B. McCulloch 1, Brad Haltli 1,2, Douglas H. Marchbank 1 and Russell G. Kerr 1,2,*

Fuente: http://mdpi.com/



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