In vitro and in vivo evaluation of C-20- and C-23-modified derivatives of tylosin against veterinary pathogens.

Abstract

Three series of semi-synthetic derivatives of tylosin-related macrolides were evaluated for utility in veterinary medicine. 23-Modified derivatives of 5-O-mycaminosyltylonolide (OMT) possessed potent activity in vitro against species of Pasteurella and Mycoplasma. An experimental infection in chicks caused by Pasteurella multocida was utilized to evaluate efficacy; several of these derivatives of OMT effectively treated the infection when given subcutaneously, but none were effective after oral administration in drinking water. Macrolides retaining the 4'-O-mycarosyl moiety (tylosin, DMT) had relatively poor activity against Pasteurella in vitro. Certain 20-modified derivatives of desmycosin demonstrated good oral bioavailability in chicks and a lead compound with oral efficacy in the Pasteurella infection model was discovered.

• Authors: H A Kirst, E E Ose, J E Toth, K E Willard, M Debono, A M Felty-Duckworth, R S Pekarek
• Journal: The Journal of antibiotics (J Antibiot (Tokyo)) Vol. 41 Issue 7 Pg. 938-48 (Jul 1988) ISSN: 0021-8820 [Print] England
• PMID: 3417566 (Publication Type: Journal Article)

Chemical References

• Leucomycins
• tylosin B
• Tylosin

Topics

• Animals
• Leucomycins (pharmacology)
• Mice
• Mycoplasma (drug effects)
• Pasteurella (drug effects)
• Pasteurella Infections (drug therapy)
• Structure-Activity Relationship
• Tylosin