Current Medicinal Chemistry - Anti-Infective Agents - Volume 4, Issue 3, 2005

The design and optimisation of the second-generation antibacterial oral streptogramin is reported in terms of semi-synthesis, structure-activity relationships, pharmaco-kinetics properties and antibacterial activities. Our endeavours led to the selection of two new combinations RPR131166/RPR132493 (30/70) and RPR202868/RPR132552 (30/70) whose antibacterial properties will be reported in detail. The overall Read More

During recent years, new extended-spectrum β-lactamase-type enzymes (ESBL) have emerged worldwide. The new enzymes, called CTX-M-type enzymes, belong to Ambler class A β-lactamases, and possess a serine in the active center of the molecule. The family of CTX-M enzymes is grouped, on the basis of similarities in amino acid sequences, into five major phylogenetic categories: the CTX-M-1 group, the CTX-M-2 g Read More

The extensive use of antimicrobials in community as well as nosocomial environments during the last half century has created a pressure that is able to select resistant microorganisms, transforming this “evolution” into one of the most dangerous phenomena of the last twenty years. Two different aspects of the same problem have to be examined: the appearance of “new opportunistic multiresistant microorganisms, and t Read More

By the early nineteen seventies the mechanism of inhibition of peptidoglycan biosynthesis by various cell wallactive antibiotics was well established, and the Gram-positive bacterium Staphylococcus aureus had often been used in the studies. From the early days of penicillin it was known that cell wall-active antibiotics are typically bactericidal causing cell death and lysis, a phenomenon that has recently been described as program Read More

Farnesyltransferase catalyzing the transfer of a farnesyl residue from farnesylpyrophosphate to the thiol of a cysteine side chain of proteins carrying the C-terminal CAAX-tetrapeptide sequence has been one of the prime targets in the development of novel anti-cancer agents. From numerous farnesyltransferase inhibitors that have been described, several have reached advanced stages of clinical trials. In addition to Read More