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US 4,727,062 AGranted
3-Halovinylglycine antibacterial agents
AssigneeMerck & Co., Inc.
InventorsDavid Taub, Robert H. Abeles, Arthur A. Patchett
Life of this patent
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Abstract
Described are 3-halovinylglycines and their amino acid dipeptide and oligopeptide conjugates, a new class of efficient antibacterial agents, pharmaceutical compositions containing them as active ingredients, and methods of synthesis. The compounds are thought to interfere in bacterial cell wall synthesis.
Claims10
A compound possessing antibacterial activity of the following formula:
- ##STR14## wherein X is halo, R.sup.1 is H, R.sup.2 is selected from H or an alpha-amino acid acyl or dipeptide acyl radical selected from the group consisting of norvalyl, norleucyl, methionyl, valyl, leucyl, 2-amino-n-butanoyl, arginyl, lysyl, phenylalanyl, seryl, tryptophanyl, 3-fluorovinylglycyl, 3-chlorovinylglycyl, norvalyl-norvalyl methinonyl-norvalyl and norleucyl-3-chlorovinylglycyl, and D, L stereoisomers and racemates thereof, excluding X=Cl, R.sup.1 =R.sup.2 =H, where the compound is a racemate.
An antibacterial pharmaceutical composition comprising a therapeutically effective amount of a compound of the following formula:
- ##STR15## wherein X is halo, R.sup.1 is H, R.sup.2 is selected from norvalyl, methionyl, and D,L stereoisomers and racemates thereof, in an acceptable pharmaceutical carrier.
Dependencies are inferred from the claim text.