Antibacterial mycaminosyl tylonolide and related macrolide derivatives
US4454314A · kind A · utility
Assignee
Inventor
Key dates
| Filing date | Aug 2, 1982 |
| Grant date | Jun 12, 1984 |
| Priority date | — |
| Expiry date | Aug 2, 2002 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P31/04
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Antibacterial and intermediate substances which are derived by selective chemical transformation of partially hydrolyzed tylosin and related macrolide derivatives in which only the mycaminose sugar remains attached to the macrocyclic lactone ring. Compounds having particular utility as antibacterial agents have C-6 side chain aldehyde converted to a hydrazone, the C-3 ring hydroxy group acylated, and/or the C-14 hydroxymethyl group converted to a sulfonate or carboxylate ester, or to a halomethyl, aminomethyl, sulfonamidomethyl or carboxamidomethyl group. Compounds whose prime utility is as intermediates have side chain aldehyde group protected as an acetal, mycaminose sugar hydroxyls protected as carboxylate ester and/or C-14 hydroxymethyl converted to a formyl or azidomethyl group.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.