Expert Opinion on Therapeutic Patents · 2000 · 31 citations · 110 references
PharmacyMedicinal ChemistryPharmacologyCombinatorial ChemistryDrug DiscoverySynthetic Medicinal ChemistryAntibacterial PharmacologyAntibiotic ResistanceAntibiotic Resistance MechanismsCombinatorial SynthesisMacrocycle SynthesisMacrocyclic Drug DesignAntibiotic DiscoveryDrug-resistant PathogensMacrocycle Library SynthesisMacrocyclic Library SynthesisMacrolide AntibioticsMacrolide Resistance MechanismsMultidrug-resistant PathogensNovel Antibacterial Drug Discovery
There have been exciting developments in the area of macrolide antibiotics recently. This activity largely stems from the discovery and development of a new class of agents called ketolides. They are more potent than erythromycin A and active against macrolide-resistant pathogens. At the same time, our knowledge of the mechanism of action of macrolides has been refined and resistance mechanisms have been elucidated. By employing new chemical methods and combinatorial biosynthesis, qualitatively different kinds of derivatives are being synthesised. Alternative non-infective uses for macrolide templates are also being explored. These areas are reviewed primarily in relation to 14-membered macrolides.
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Modular Organization of Genes Required for Complex Polyketide Biosynthesis
Stefano Donadio, Michael J. Staver, James B. McAlpine et al. · Science · 1991 · 909 citations