GB1439878A - Penicillins - Google Patents

Abstract

1439878 N-alkoxy-ureido-penicillin BEECHAM GROUP Ltd 19 Dec 1974 [29 Dec 1973] 60155/73 Heading C2C Novel compounds of Formula (I) or pharmaceutically acceptable salts or esters thereof, where R is phenyl or amino-, hydroxy- or halo-substituted phenyl, a monocyclic 5 to 7 membered heterocyolic radical, C 1-7 alkyl, 3 to 7 membered cycloalkyl or cyclohexadienyl; R<SP>3</SP> is H or R and R<SP>3</SP> together form a 5 to 7 membered cycloalkyl or heterocyclic ring; and R<SP>1</SP> and R<SP>2</SP> are the same or different and each is hydrogen, C 1-7 alkyl, phenyl, phenylalkyl or amino-, hydroxy- or halo-substituted phenyl phenyl or phenylalkyl, 5 to 7 membered cycloalkyl or a monocyclic 5 to 7 membered heterocyclic radical, may be obtained by reacting a 6- amino-penicillanic acid or a salt, ester or silyl derivative thereof with a reactive N-acylating derivative of an acid of the Formula (II) or by reacting a compound of Formula (III) or a salt or ester or silyl derivative thereof, wherein any free amino groups are protected with a compound of formula where X is a halogen atom, and removing any silyl groups by hydrolysis or alcoholysis, and removing any amino protecting groups, and optionally converting any ester to a free acid or salt, or another ester. The new penicillins are useful as antibacterial agents, as nutritional supplements in animal foods, as agents for treatment of mastitis in cattle and as therapeutic agents against infectious diseases caused by Gram negative and Gram positive bacteria, and may be used in pharmaceutical compositions together with one or more pharmaceutically acceptable carriers.