Issue 10, 2014

Non-classical β-carbonic anhydrase inhibitors-towards novel anti-mycobacterials

Abstract

Mycobacterial carbonic anhydrases, such as the essential protein Rv3588c, are attractive drug targets since they constitute a different class of carbonic anhydrases than those found in humans. A natural product library has been screened for compounds that inhibit mycobacterial carbonic anhydrases but lack the much-exploited sulfonamide/sulfamate group. The identified inhibitors of mycobacterial Rv3588c are likely to affect the enzyme at a site different from the catalytic centre – a concept which may be exploited for novel specific anti-mycobacterials.

Graphical abstract: Non-classical β-carbonic anhydrase inhibitors-towards novel anti-mycobacterials

Supplementary files

Article information

Article type
Concise Article
Submitted
18 Jul 2014
Accepted
10 Aug 2014
First published
12 Aug 2014

Med. Chem. Commun., 2014,5, 1563-1566

Author version available

Non-classical β-carbonic anhydrase inhibitors-towards novel anti-mycobacterials

N. von Gnielinski, L. Nienaber, L. Mason, S. Ellis, J. A. Triccas, R. A. Davis and A. Hofmann, Med. Chem. Commun., 2014, 5, 1563 DOI: 10.1039/C4MD00310A

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