Design,synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase |
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Authors: | David H McGarry Ian R Cooper Rolf Walker Catherine E Warrilow Mark Pichowicz Andrew J Ratcliffe Anne-Marie Salisbury Victoria J Savage Emmanuel Moyo John Maclean Andrew Smith Cédric Charrier Neil R Stokes David M Lindsay William J Kerr |
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Institution: | 1. Redx Pharma, Alderley Park, Cheshire SK10 4TG, United Kingdom;2. Department of Pure and Applied Chemistry, University of Strathclyde, WestCHEM, Thomas Graham Building, 295 Cathedral Street, Glasgow G1 1XL, United Kingdom |
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Abstract: | According to the World Health Organization (WHO), approximately 1.7 million deaths per year are caused by tuberculosis infections. Furthermore, it has been predicted that, by 2050, antibacterial resistance will be the cause of approximately 10 million deaths annually if the issue is not tackled. As a result, novel approaches to treating broad-spectrum bacterial infections are of vital importance. During the course of our wider efforts to discover unique methods of targeting multidrug-resistant (MDR) pathogens, we identified a novel series of amide-linked pyrimido4,5-b]indol-8-amine inhibitors of bacterial type II topoisomerases. Compounds from the series were highly potent against gram-positive bacteria and mycobacteria, with excellent potency being retained against a panel of relevant Mycobacterium tuberculosis drug-resistant clinical isolates. |
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Keywords: | ESKAPE pathogens Anti-infectives Topoisomerases DNA gyrase Corresponding author |
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