1.
J Med Chem
; 53(10): 3927-36, 2010 May 27.
Article
in English
| MEDLINE
| ID: mdl-20426423
ABSTRACT
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.
Subject(s)
Anti-Bacterial Agents/chemical synthesis , Bacterial Proteins/antagonists & inhibitors , Cytoskeletal Proteins/antagonists & inhibitors , Pyridines/chemical synthesis , Staphylococcus aureus/drug effects , Thiazoles/chemical synthesis , Animals , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Biological Availability , Blood Proteins/metabolism , Caco-2 Cells , Cell Division/drug effects , Cell Membrane Permeability , Hepatocytes/metabolism , Humans , Mice , Microbial Sensitivity Tests , Models, Molecular , Protein Binding , Pyridines/chemistry , Pyridines/pharmacology , Staphylococcal Infections/drug therapy , Staphylococcus aureus/cytology , Structure-Activity Relationship , Thiazoles/chemistry , Thiazoles/pharmacology
2.
Bioorg Med Chem Lett
; 19(2): 524-7, 2009 Jan 15.
Article
in English
| MEDLINE
| ID: mdl-19064318
ABSTRACT
3-Methoxybenzamide is a weak inhibitor of the essential bacterial cell division protein FtsZ. Exploration of the structure-activity relationships of 3-methoxybenzamide analogues led to the identification of potent anti-staphylococcal compounds.
