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US 4,048,431 AGranted
Alkylated derivatives of antibiotic BM123.gamma.
AssigneeAmerican Cyanamid Company
InventorsJoseph John Hlavka, Panayota Bitha
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Abstract
This disclosure describes a novel series of potent antibacterial agents derived by reductive alkylation of antibiotic BM123.gamma. with certain classes of aldehydes and ketones.
Claims36
A compound selected from the group consisting of those of the formulae:
- ##STR6## wherein R is a moiety selected from the group consisting of those of the formulae:
- ##STR7## R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, halo substituted lower alkyl, lower alkenyl, phenyl, acetamidophenyl, nitrophenyl, mercaptophenyl, anisyl, tolyl, phenyl lower alkyl, 2-furyl, methyl substituted 2-furyl, 2thienyl, methyl substituted 2-thienyl, 2-pyrryl, methyl substituted 2-pyrryl, 2-pyridyl and 2-quinolyl;
- and the pharmacologically acceptable acid-addition salts thereof.
A compound selected from the group consisting of those of the formula:
- ##STR8## wherein R is a moiety selected from the group consisting of those of the formulae:
- ##STR9## R.sub.2 is selected from the group conisting of lower alkyl, halo substituted lower alkyl and phenyl lower alkyl;
- R.sub.3 is selected from the group consisting of lower alkyl, halo substituted lower alkyl, lower alkenyl, lower cycloalkyl, phenyl, acetamidophenyl, nitrophenyl, mercaptophenyl, anisyl, tolyl, phenyl lower alkyl, acetamidophenyl lower alkyl, nitrophenyl lower alkyl, mercaptophenyl lower alkyl, anisyl lower alkyl and tolyl lower alkyl;
- and R.sub.2 and R.sub.3 taken together with the associated methylidyne group is cyclopentyl, mono-lower alkyl substituted cyclopentyl, di-lower alkyl substituted cyclopentyl, tri-lower alkyl substituted cyclopentyl, cyclohexyl, mono-lower alkyl substituted cyclohexyl, di-lower alkyl substituted cyclohexyl or tri-lower alkyl substituted cyclohexyl;
- and the pharmacologically acceptable acid-addition salts thereof.
2 more elements
Dependencies are inferred from the claim text.