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[摘要]：Importance of the field: Nosocomial infections caused by multi-drug resistant (MDR) Gram-negative bacteria are on the increase, often with few or no therapeutic options for treatment. Historically, a successful approach to generate novel antibiotics has been the chemical modification of existing classes, addressing deficiencies such as resistance mechanisms, safety profile or pharmacokinetic parameters. Aminoglycosides (AGs) represent one of the five clinically-used classes (AGs, beta-lactams, quinolones, tetracyclines and sulfonamides) with activity against Gram-negative bacteria. Areas covered in this review: A summary of the AG patent literature between the beginning of 2005 and February 2010 with the main focus on novel AG analogs with potential for therapeutic activity against MDR Gram-negative pathogens. What the reader will gain: Overview of the patent literature in the aminoglycoside field during the past 5 years including an assessment of the therapeutic potential for the derivatives described. Take home message: A few companies and academic groups have recently reawakened the dormant field of AG antibiotics, successfully applying novel technologies. So far, this has yielded one clinical candidate, ACHN-490, currently undergoing a Phase II evaluation in complicated urinary tract infections. |
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