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Chapter 12. Antibacterial Agents

1994; Elsevier BV; Linguagem: Inglês

10.1016/s0065-7743(08)60725-3

1557-8437

Martin R. Jefson, Scott J. Hecker, John P. Dirlam,

Antibiotic Resistance in Bacteria

El101, the isopropoxycarbonyloxyethyl ester prodrug of El100, exhibits good oral absorption, and has potent activity against susceptible strains. Among carbapenems, most new agents contain the 18-methyl group that has been found to impart good stability to renal dehydropeptidase I. The majority of the currently marketed quinolones, such as ciprofloxacin, contain a piperazine or substituted piperazine at the 7-position. These agents are used for a broad variety of clinical indications, such as respiratory tract, urinary tract, skin and soft tissue, bone, and sexually transmitted diseases. Methyl substitution on the pyrrolidine ring is found to improve the solubility and, therefore, provide a better pharmacokinetic profile. Mechanism of action studies against E. coli suggest that, while intact cephalosporin 3'-quinolone esters act as cephalosporins, carbarnates and amines may possess both cephalosporin and quinolone activity in the intact molecule. The 8a-azalides exhibit improved acid stability and comparable activity in mouse infection models. Glycylcycline is a new series of tetracycline derivatives, found to have a broad spectrum of activity against tetracycline susceptible and resistant bacteria, including strains containing ribosomal protection resistance determinants. Some of these analogs exhibit good activity against streptococcal and enterococcal strains that are resistant to vancomycin. Replacement of the dehydrofucose sugar moiety, with an allyl group, affords activity comparable to that of the natural product.