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Creating an Antibacterial with in Vivo Efficacy: Synthesis and Characterization of Potent Inhibitors of the Bacterial Cell Division Protein FtsZ with Improved Pharmaceutical Properties
Author(s) -
David J. Haydon,
James M. Bennett,
David R. Brown,
Ian Collins,
Greta Galbraith,
Paul Lancett,
Rebecca Macdonald,
Neil R. Stokes,
Pramod K. Chauhan,
Jignesh K. Sutariya,
Narendra Nayal,
Anil Srivastava,
Joy Beanland,
Robyn N. Hall,
Vincent Henstock,
Caterioula,
Chris Rockley,
Lloyd G. Czaplewski
Publication year - 2010
Publication title -
journal of medicinal chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.01
H-Index - 261
eISSN - 1520-4804
pISSN - 0022-2623
DOI - 10.1021/jm9016366
Subject(s) - ftsz , chemistry , in vivo , bacterial cell structure , cell division , antibacterial activity , in vitro , bacterial protein , antibacterial agent , cell , drug , alkyl , division (mathematics) , biochemistry , bacteria , combinatorial chemistry , antibiotics , pharmacology , biology , organic chemistry , genetics , gene , arithmetic , mathematics
3-Methoxybenzamide (1) is a weak inhibitor of the essential bacterial cell division protein FtsZ. Alkyl derivatives of 1 are potent antistaphylococcal compounds with suboptimal drug-like properties. Exploration of the structure-activity relationships of analogues of these inhibitors led to the identification of potent antistaphylococcal compounds with improved pharmaceutical properties.

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