| Abstract | Natural products have played a pivotal role in antibiotic drug discovery with most antibacterial drugs being derived from a natural product or natural product lead. However, the rapid onset of resistance to most antibacterial drugs diminishes their effectiveness considerably and necessitates a constant supply of new antibiotics for effective treatment of infections. The natural product templates of actinonin, pleuromutilin, ramoplanin and tiacumicin B, which are compounds undergoing clinical evaluation, represent templates not found in currently marketed antibacterial drugs. In addition, the new templates present in the recently discovered lead antibacterials arylomycin, GE23077, mannopeptimycin, muraymycin/caprazamycin, nocathiacin and ECO-0501, are discussed. Despite extensive efforts to identify antibiotic leads from molecular targets, only the peptide deformylase inhibitor LBM-415 is currently in clinical trials. It is proposed that new antibacterial assays which combine cell-based screening with molecular targets could offer better prospects for lead discovery. |
| Authors | Mark S Butler, Antony D Buss
(Affiliation: MerLion Pharmaceuticals, 1 Science Park Road, The Capricorn #05-01, Singapore Science Park II, Singapore 117528, Singapore. mark at merlionpharma.com)
|
| Journal | Biochemical pharmacology
(Biochem Pharmacol)
Vol. 71
Issue 7
Pg. 919-29
(Mar 30 2006)
ISSN: 0006-2952 England |
| PMID | 16289393
(Publication Type: Journal Article, Review)
|
| Chemical References |
- Anti-Bacterial Agents
- Biological Products
|
| Topics |
- Anti-Bacterial Agents
(chemistry, pharmacology)
- Biological Products
(chemistry, pharmacology)
- Drug Design
- Drug Industry
(trends)
- Drug Resistance, Multiple, Bacterial
(drug effects)
- Humans
- Molecular Structure
|
