J. Bronson, J. Barrett
2001
Citations
0
Influential Citations
6
Citations
Journal
Annual Reports in Medicinal Chemistry
Abstract
Publisher Summary This chapter examines the various developments in antibacterial research. Significant effort continues to be devoted to the research, development, and marketing of novel antibacterial agents. Linezolid was approved by the US FDA for treatment of patients with infections caused by Gram-positive bacteria. Approved indications include nosocomial pneumonia, community-acquired pneumonia, complicated and uncomplicated skin and skin structure infections, and vancomycin-resistant enterococcus infections caused by methicillin resistant Staphylococcus aureus (MRSA). Azamulin has excellent potency against Gram-positive and some Gram-negative bacteria; however development was discontinued after Phase I trials. The main liabilities in the pleuromutilin class are susceptibility to metabolism, moderate bioavailability, and potent cytochrome P450 inhibition for some derivatives. The BMS-247243 is a novel parenteral cephalosporin derivative with excellent activity against Gram-positive bacteria. BMS-247243 has good potency against MRSA, with an MIC 90 of 4 μg/mL. Among the most advanced parenteral carbapenems in development is MK-826, a broad spectrum parenteral derivative with a significant pharmacokinetic advantage over other carbapenems in that it can be administered once daily.