Chemistry of pseudomonic acid. Part 16. Aryl and heteroaryl ketone derivatives of monic acid

A Abson; N J Broom; P A Coates; J S Elder; A K Forrest; P C Hannan; A J Hicks; P J O'Hanlon; N D Masson; N D Pearson; J E Pons; J M Wilson

doi:10.7164/antibiotics.49.390

Chemistry of pseudomonic acid. Part 16. Aryl and heteroaryl ketone derivatives of monic acid

J Antibiot (Tokyo). 1996 Apr;49(4):390-4. doi: 10.7164/antibiotics.49.390.

Authors

A Abson¹, N J Broom, P A Coates, J S Elder, A K Forrest, P C Hannan, A J Hicks, P J O'Hanlon, N D Masson, N D Pearson, J E Pons, J M Wilson

Affiliation

¹ SmithKline Beecham Pharmaceuticals, Brockham Park, Betchworth, Surrey, UK.

PMID: 8642004
DOI: 10.7164/antibiotics.49.390

Abstract

The synthesis, antibacterial activities, murine pharmacokinetic and infection model data for a range of aryl and heteroaryl ketone derivatives of monic acid (2a) are reported. The best results were found for the 3-furyl and 2-methoxy thiazol-5-yl analogues.

MeSH terms

Animals
Anti-Bacterial Agents / chemistry*
Anti-Bacterial Agents / pharmacokinetics
Anti-Bacterial Agents / pharmacology*
Humans
Ketones / chemistry
Male
Mice
Mice, Inbred Strains
Microbial Sensitivity Tests
Mupirocin / analogs & derivatives*
Mupirocin / chemistry*
Mupirocin / pharmacology
Sepsis / drug therapy
Staphylococcal Infections / drug therapy
Structure-Activity Relationship
Thiazoles / chemistry

Substances

Anti-Bacterial Agents
Ketones
Thiazoles
Mupirocin