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13 results on '"Christoff, Rebecca M."'

10. Enhancing allosteric inhibition of dihydrodipicolinate synthase through the design and synthesis of novel dimeric compoundsElectronic supplementary information (ESI) available. CCDC 2235014–2235016. For ESI and crystallographic data in CIF or other electronic format see DOI: https://doi.org/10.1039/d3md00044c

Author

Christoff, Rebecca M., Al Bayer, Mohammad, Soares da Costa, Tatiana P., Perugini, Matthew A., and Abbott, Belinda M.

Abstract

The synthesis of the first dimeric inhibitor of E. colidihydrodipicolinate synthase (DHDPS) is reported herein. Inspired by 2,4-thiazolidinedione based ligands previously shown to inhibit DHDPS, a series of dimeric inhibitors were designed and synthesised, incorporating various alkyl chain bridges between two 2,4-thiazolidinedione moieties. Aiming to exploit the multimeric nature of this enzyme and enhance potency, a dimeric compound with a single methylene bridge achieved the desired outcome with low micromolar inhibition of E. coliDHDPS observed. This work highlights the continued importance of investigation into DHDPS as an antibacterial target. Furthermore, we demonstrate the design of dimeric ligands can provide a promising strategy to improve potency in the search for novel bioactive compounds.

Published
2023
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13. Antimalarial activity of novel 4-cyano-3-methylisoquinoline inhibitors against Plasmodium falciparum: design, synthesis and biological evaluation

Author

Buskes, Melissa J., primary, Harvey, Katherine L., additional, Richards, Benjamin J., additional, Kalhor, Robabeh, additional, Christoff, Rebecca M., additional, Gardhi, Chamodi K., additional, Littler, Dene R., additional, Cope, Elliott D., additional, Prinz, Boris, additional, Weiss, Greta E., additional, O'Brien, Nathan J., additional, Crabb, Brendan S., additional, Deady, Leslie W., additional, Gilson, Paul R., additional, and Abbott, Belinda M., additional

Published
2016
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