Dichloro-naphthoquinone as a non-classical inhibitor of the mycobacterial carbonic anhydrase Rv3588c12. Issue 6 (18th May 2017)

• Record Type: Journal Article
• Authors: Dallaston, M. A.; Rajan, S.; Chekaiban, J.; Wibowo, M.; Cross, M.; Coster, M. J.; Davis, R. A.; Hofmann, A.
• Is Part Of: MedChemComm. Volume 8:Issue 6(2017)
• Page Start: 1318
• Page End: 1321
• Publication Date: 2017-05-18
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19
• DOI: 10.1039/c7md00090a
• Languages: English
• ISSNs: 2040-2503

Abstract

Abstract : This study reports the most active non-sulfonamide mycobacterial CA inhibitor to date. Abstract : The soluble mycobacterial carbonic anhydrases Rv3588c and Rv1284 belong to a different class of carbonic anhydrases than those found in humans, making them attractive drug targets by using the inherent differences in the folds of the different classes. By screening a natural product library, we identified naphthoquinone derivatives as a novel non-classical inhibitor scaffold of mycobacterial carbonic anhydrases that lack the sulfonamide/sulfamate group and thus did not affect human carbonic anhydrase II.