PHOSPHORUS CONTAINING PEPTIDE DERIVATIVES, THEIR PRODUCTION, INTERMEDIATES FOR THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

摘要

Peptide derivatives provided by the present invention are compounds of the general formula wherein R1 represents a hydrogen atom or the methyl or hydroxymethyl group or a mono-, di- or trihalomethyl mgroup; R2 represents the characterizing group of an alpha -amino acid of the type normally found in proteins or a lower alkyl or hydroxy- (lower alkyl) group other than the characterising group of an alpha -amino acid of the type normally found in proteins; R3 represents a lower alkyl, lower cycloalkyl, lower alkenyl, aryl or aryl-(lower alkyl) group; R4 represents a hydrogen atom or a lower alkyl group; n stands for 1,2 or 3; the configuration at the carbon atom designated as (a) is (R) when R1 represents other than a hydrogen atom and the configuration at the carbon atom designated as (b) is (L) when R2 represents other than a hydrogen atom, and pharmaceutically acceptable salts thereof. The compounds exhibit activity as antibacterial agents against a range of gram-positive and gram-negative bacteria. Also disclosed are intermediates and a process for the production of the end product.