title: Structure-activity studies of 20-deoxo-20-amino derivatives of tylosin-related macrolides.
abstract: Reductive amination of the C-20 aldehyde group of tylosin and related macrolides yielded a large series of derivatives with potentially useful antibiotic properties. Evaluation of these new compounds was conducted on the basis of: 1) Broad antimicrobial spectrum in vitro, with particular emphasis on inhibition of Pasteurella multocida and Pasteurella haemolytica; 2) in vivo efficacy, especially when given orally, against P. multocida in experimental infections in chicks; and 3) bioavailability after oral administration to laboratory animals. The most useful activity was found within a series of derivatives produced by reductive amination of desmycosin with secondary amines.
authors.affiliation: Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285.
authors.forename: H A
authors.initials: HA
authors.lastname: Kirst
authors.forename: K E
authors.initials: KE
authors.lastname: Willard
authors.forename: M
authors.initials: M
authors.lastname: Debono
authors.forename: J E
authors.initials: JE
authors.lastname: Toth
authors.forename: B A
authors.initials: BA
authors.lastname: Truedell
authors.forename: J P
authors.initials: JP
authors.lastname: Leeds
authors.forename: J L
authors.initials: JL
authors.lastname: Ott
authors.forename: A M
authors.initials: AM
authors.lastname: Felty-Duckworth
authors.forename: F T
authors.initials: FT
authors.lastname: Counter
authors.forename: E E
authors.initials: EE
authors.lastname: Ose
mesh_terms: D000586:Amination; D000818:Animals; D002645:Chickens; D051379:Mice; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D010084:Oxidation-Reduction; D010325:Pasteurella / Q000187:drug effects*; D010326:Pasteurella Infections / Q000188:drug therapy; D013290:Streptococcal Infections / Q000188:drug therapy; D013297:Streptococcus pyogenes / Q000187:drug effects; D013329:Structure-Activity Relationship; D015645:Tylosin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D015645:Tylosin