ABSTRACT
Oxazolidinones possessing a C-5 carboxamide functionality (reverse amides) represent a new series of compounds that block bacterial protein synthesis. These reverse amides also exhibited less potency against monoamine oxidase (MAO) enzymes and thus possess less potential for the side effects associated with MAO inhibition. The title compound (14) showed reduced in vivo myelotoxicity compared to linezolid in a 14-day safety study in rats, potent in vivo efficacy in murine systemic infection models, and excellent pharmacokinetic properties.
Subject(s)
Anti-Bacterial Agents/chemical synthesis , Cyclic S-Oxides/chemical synthesis , Oxazolidinones/chemical synthesis , Acetamides/pharmacology , Administration, Oral , Animals , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/toxicity , Biological Availability , Cyclic S-Oxides/pharmacology , Cyclic S-Oxides/toxicity , Dogs , Drug Resistance, Bacterial , Female , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/drug effects , Injections, Intravenous , Linezolid , Male , Mice , Microbial Sensitivity Tests , Monoamine Oxidase Inhibitors/chemical synthesis , Monoamine Oxidase Inhibitors/pharmacology , Monoamine Oxidase Inhibitors/toxicity , Oxazolidinones/pharmacology , Oxazolidinones/toxicity , Rats , Rats, Sprague-Dawley , Staphylococcal Infections/drug therapy , Staphylococcus aureus , Streptococcal Infections/drug therapy , Streptococcus pyogenes , Structure-Activity RelationshipABSTRACT
OBJECTIVE:To observe the therapeutic efficacy and safety of polyene phosphatidyl choline and atorvastatin in the treatment of alcoholic liver disease. METHODS:112 patients with alcoholic liver disease were randomly divided into control group (n=56)and treatment group(n=56). Both groups were given a cure for alcoholism,vitamin and polyene phosphatidyl choline (465mg,qd,i.v. gtt)therapy. Treatment group were additionally treated with torvastatin(10 mg,po)once a day before bed for 4 weeks. Clinical symptoms,signs,liver function,blood lipid changes of two groups before and after treatment were observed. RESULTS:Treatment group was superior to control group in respect of clinical symptoms,signs,liver function and blood lipid changes(P
