C - Chemistry – Metallurgy – 07 – F
Patent
C - Chemistry, Metallurgy
07
F
260/501, 530/5.0
C07F 9/28 (2006.01) A61K 31/66 (2006.01) C07F 9/30 (2006.01) C07F 9/38 (2006.01) C07K 5/06 (2006.01) C08G 69/10 (2006.01) A61K 38/00 (2006.01)
Patent
CA 1065857
ABSTRACT The present invention relates to the preparation of peptide derivatives of the general formula Image (I) , wherein R1 represents a hydrogen atom or a lower alkyl, lower cycloalkyl, (lower cycloalkyl)-(lower alkyl), aryl or aryl- (lower alkyl) group (said groups being optionally substituted as the case may require by one or more amino, hydroxy, thio, methylthio, carboxy or guanidino groups so as to form the characterising group of a naturally occurring L .alpha.-amino acid); R2 and R3 each represent the characterising group of an .alpha.-amino acid of the type normally found in proteins with the proviso that R3 cannot represent a hydrogen atom when n is zero and R1 is a hydrogen atom or the phenyl group; R4 represents a hydroxy or methyl group; n stands for zero, 1, 2 or 3; the single asterisks denote that the configuration at the carbon atom so-marked is L; and the double asterisk denotes that, when R1 represents other than a hydrogen atom, the configuration at the carbon atom so-marked is R, and of their pharmaceutically acceptable salts. These compounds possess antibacterial activity and potentiate the activity of antibiotics.
244191
Atherton Frank R.
Hall Michael J.
Hassall Cedric H.
Lambert Robert W.
Ringrose Peter S.
Hoffmann-La Roche Limited
Na
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