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The rise of antibiotic resistance, especially in staphylococcus aureus, and the increasing death rate due to multi-resistant bacteria have been well documented. The need for new chemical entities and/or the identification of novel targets for antibacterial drug development is high. Lipoteichoic acid (LTA), a membrane attached anionic polymer, is important for the growth and virulence of many Gram-positive bacteria and interest has been high in the discovery of LTA biosynthesis inhibitors. Thus far only a handful of LTA biosynthesis inhibitors have been described with moderate (MIC = 5.34 µg/mL) to low (MIC = 1024 µg/mL) activities against S. aureus. Here we describe the identification of novel compounds that potently inhibit LTA biosynthesis in S. aureus, displaying impressive antibacterial activities (MIC as low as 0.25 µg/mL) against methicillin-resistant S. aureus (MRSA). Under similar in-vitro assay conditions, these compounds are 4X more potent than vancomycin and 8X more potent than Linezolid against MRSA.
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A strain of Staphylococcus aureus that is non-susceptible to the action of METHICILLIN. The mechanism of resistance usually involves modification of normal or the presence of acquired PENICILLIN BINDING PROTEINS.
A 25-kDa peptidase produced by Staphylococcus simulans which cleaves a glycine-glcyine bond unique to an inter-peptide cross-bridge of the STAPHYLOCOCCUS AUREUS cell wall. EC 220.127.116.11.
Pneumonia caused by infections with bacteria of the genus STAPHYLOCOCCUS, usually with STAPHYLOCOCCUS AUREUS.
A species of STAPHYLOCOCCUS similar to STAPHYLOCOCCUS HAEMOLYTICUS, but containing different esterases. The subspecies Staphylococcus hominis novobiosepticus is highly virulent and novobiocin resistant.
Potentially pathogenic bacteria found in nasal membranes, skin, hair follicles, and perineum of warm-blooded animals. They may cause a wide range of infections and intoxications.
MRSA (methicillin-resistant Staphylococcus aureus)
MRSA (methicillin-resistant Staphylococcus aureus) is a family of bacteria with resistance to one or more major antibiotics. There are currently 17 different strains of MRSA. Two particular strains, EMRSA15 and EMRSA16 account for 96% of MRSA blood...
Clinical Approvals Clinical Trials Drug Approvals Drug Delivery Drug Discovery Generics Drugs Prescription Drugs In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which drugs are dis...