Creating an Antibacterial with in Vivo Efficacy: Synthesis and Characterization of Potent Inhibitors of the Bacterial Cell Division Protein FtsZ with Improved Pharmaceutical Properties

Autor:	JamesM. Bennett, Ian Collins, Lloyd George Czaplewski, David J. Haydon, Rebecca Macdonald, Pramod K. Chauhan, David A. Brown, Vincent Henstock, Neil R. Stokes, Greta Galbraith, Robin Hall, Anil K Srivastava, Paul Lancett, Joy Beanland, Caterina Noula, Narendra Nayal, Jignesh K. Sutariya, Chris Rockley
Rok vydání:	2010
Předmět:	Models Molecular Staphylococcus aureus Cell Membrane Permeability Cell division Pyridines Biological Availability Microbial Sensitivity Tests Plasma protein binding 01 natural sciences Article Bacterial cell structure Mice Structure-Activity Relationship 03 medical and health sciences Bacterial Proteins In vivo Drug Discovery Animals Humans Structure–activity relationship Cytoskeleton FtsZ 030304 developmental biology 0303 health sciences biology 010405 organic chemistry Chemistry Blood Proteins Staphylococcal Infections Anti-Bacterial Agents 3. Good health 0104 chemical sciences Cytoskeletal Proteins Thiazoles Biochemistry Caco-2 Hepatocytes biology.protein Molecular Medicine Caco-2 Cells Cell Division Protein Binding
Zdroj:	Journal of Medicinal Chemistry
ISSN:	1520-4804 0022-2623
DOI:	10.1021/jm9016366
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::14b0617fb320dd9003dcf03b3aefd312 https://doi.org/10.1021/jm9016366 Zobrazit plný text záznamu