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Antibiotics from gliding bacteria, XLII. Chemical modification of sorangicin A and structure — Activity relationship I: Carboxyl and hydroxyl group derivatives
Author(s) -
Jansen Rolf,
Schummer Dietmar,
Irschik Herbert,
Höfle Gerhard
Publication year - 1990
Publication title -
liebigs annalen der chemie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 0170-2041
DOI - 10.1002/jlac.1990199001178
Subject(s) - chemistry , bacteria , antibiotics , in vitro , escherichia coli , staphylococcus aureus , rna polymerase , chemical modification , structure–activity relationship , combinatorial chemistry , stereochemistry , biochemistry , gene , biology , genetics
Abstract The synthesis of selectively protected sorangicin A derivatives and their application in the modification of the hydroxyl groups and the carboxyl group in sorangicin A ( 1 ) is described. Esters, amides, and sorangicins modified at the hydroxyl groups were prepared and their activities against Staphylococcus aureus, Escherichia coli , and their in vitro inhibition of RNA polymerase were examined. Although no sorangicin A derivatives with superior biological activity were observed, some derivatives completely retained their antibiotic activity or were slightly improved in their activity with certain strains.