Antibiotic cephalosporin cpds.

摘要

Cehalosporin derivatives of the general formula (I): where R = hydrogen, or a group of formula (II), (III), (IV), (V), or (VI). In (II), X = protected amino, hydroxy, C1-C3 alkoxy, -COOH, or C1-C3 alkanoyl group. In formula (III), X = sulphur, oxygen, or a chemical bond, y = 0-2, z = 1-3. In (II), (III) and (IV), Q = hydrogen, C1-C3 alkyl, or alkoxy, cyano, nitro, hydroxy, chlorine, - bromine, fluorine, trifluoromethyl, -amino-(C1-C3)-alkyl, carboxymethyl (HOOC-CH2-) or carboxamidomethyl (H2NC(O)CH2-). In (V), X = oxygen or sulphur, and Z = hydrogen or together form another benzene ring. In figure (VI), R1 and R2 = hydrogen, methyl, 2- sydnone-3-(C1-C3)-alkanoyl group, (C1-C10)alkanoyl group, (C3-C10) alkenoyl group, (C1-C7)-alkyl-X-(C1-C3)-alkanoyl group (in which X = O or S), (C3-C7)-alkenyl-X-(C1-C3)-alkanoyl group (where X = O or S), (C2-C10)-halogenalkanoyl group (where the halogen is fluorine, chlorine or bromine), or a C2-C10 cyanoalkyl group, also In (I) R' = cyano group or the group OY where Y = C1-C10 alkyl, C3-C10 alkenyl, C3-C10 alkynyl, C5-C7 cycloalkyl, (C5-C7)-cycloalkyl-(C1-C3)-alkyl, C2-C10 haloalkyl, or a (C3-C10)-haloalkenyl or haloalkynyl group in which the halogen is bromine, chlorine, fluorine or iodine, a (C1-C3)-alkyl-X-(C1-C6)-alkyl (where X = O or S), (C2-C4)-alkanoyloxy (C1-C6)-alkyl, (C2-C4)-alkanoyl-(C1-C6)-alkyl, 2'-furyl (C1-C3)-alkyl, (2'-thienyl)-(C1-C3)-alkyl, 3'-tetrahydrofuryl, tetrahydrofuryl-(C1-C3)-alkyl, or by a phenyl, benzyl or phenylethyl group which may be substituted by either a (C1-C3)-alkyl, a (C1-C3)-alkoxy, (C1-C3)-alkoxycarbonyl, a fluorine, chlorine, bromine, nitro, cyano, or trifluoromethyl group. R" = hydrogen, a zwitterion charge, a salt with a pharmaceutically acceptable cation, a C4-C6 tert. alkyl group, a C5-C7 tert. alkenyl group, A C5-C7 tert. alkynyl group, a benzyl, benzhydryl, phthalimidomethyl, methoxybenzyl, nitrobenzyl, succinimidomethyl, trimethylsilyl or a phenacyl ester group. Antibiotics.