Review Article

Antibacterial Discovery and Development: From Gene to Product and Back

Table 1

Examples of natural products (NP), semisynthetic modified natural products (SNP), natural product-derived but produced by chemical synthesis (NP-derived), or totally synthetic antibiotics (S) launched since 2000: production method, chemical class, activity against Gram-positive and/or Gram-negative bacteria, lead source, and producing organism.

ProductionClassNP-lead sourceLead sourceAntibacterial spectrum Drug nameYear approved

Chemical synthesisOxazolidinoneSG+Linezolid2000

Fed-batch fermentationLipopeptideActinomycete
(Streptomyces roseosporus)
SNP (A21978C)G+Daptomycin2003

Chemical synthesis CarbapenemNP-derivedG+/G−Doripenem2005

Fed-batch fermentationPleuromutilinFungus
(Pleurotus spp.)
SNP (pleuromutilin)G+Retapamulin2007

Fed-batch fermentation GlycopeptideActinomycete
(Amycolatopsis spp.)
SNP (vancomycin)G+Telavancin 2009

Fed-batch fermentation-lactamFungus
(Cephalosporium acremonium)
SNP (cephalosporin)G+/G−Ceftaroline fosamil2010

Fed-batch fermentation TiacumicinActinomycete
(Dactylosporangium aurantiacum)
NPG+Fixadomicin2011

Fed-batch fermentation Glycopeptide Actinomycete
(Nonomuraea sp.)
SNP (A40926)G+Dalbavancin2014