Importance

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Abstract

Compounds of the general formula I 1 wherein R.sub.1 is hydrogen, halogen, CH.sub.3, CH.sub.2--OH, COOH, CH.sub.2--OSO.sub.3, CH.sub.2--NH(CH.sub.2).sub.a--R.sub.10, or C(.dbd.O)--NH--(CH.sub.2).sub.a--R.sub.10 wherein R.sub.10 is --NH.sub.2, --NH--(CH.sub.2).sub.b--NH.sub.2, --NH--(CH.sub.2).sub.b--NH--(CH.sub.2).-sub.c--NH.sub.2, --NH--(CH.sub.2).sub.b--NH--(CH.sub.2).sub.c--NH--(CH.sub-.2).sub.d--NH.sub.2, --NH--(CH.sub.2).sub.b--NH--(CH.sub.2).sub.c--NH--(CH-.sub.2).sub.d--NH(CH.sub.2).sub.e--NH.sub.2, --NH--(CH.sub.2).sub.b--NH--(-CH.sub.2)O--NH--(CH.sub.2).sub.d--NH--(CH.sub.2).sub.e--NH--(CH.sub.2).sub-.f--NH.sub.2, a saturated or unsaturated heterocyclic ring comprising 1 or 2 heteroatoms, or --NH--(CH.sub.2).sub.b--R.sub.11, wherein R.sub.11 is a saturated or unsaturated heterocyclic ring comprising 1 or 2 heteroatoms, and a, b, c, d, e and f are the same or different and individually represent integers of from 1 to 5; R.sub.2 is hydrogen, halogen, --OH or --OR.sub.12, wherein R.sub.12 is SO.sub.3, C.sub.1-6 alkyl or C.sub.1-6 acyl, --NH--(CH.sub.2).sub.a--R.su-b.10; R is hydrogen, halogen, a lipophilic group, --NH.sub.2--(CH.sub.2).sub.a---R.sub.10 or CH.sub.2--NH--(CH.sub.2).sub.a--R.sub.10; R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.9 are the same or different and individually represent hydrogen, halogen, --OH, --OSO.sub.3 or --NH--(CH.sub.2).sub.a--R.sub.10; R.sub.3 and R.sub.8 are the same or different and individually represent hydrogen, halogen, --OH or OSO.sub.3; and the dotted lines between carbon atoms 1 and 2, 13 and 17, 16 and 17, and 17 and 20 indicate the presence of a single or double bond; provided that at least one and not more than two of R, R.sub.1, R.sub.2, R.sub.4, R.sub.5, R.sub.6, R.sub.7 or R.sub.9 is --NH--(CH.sub.2).sub.a---R.sub.10, CH.sub.2--NH--(CH.sub.2).sub.a--R.sub.10 or C(.dbd.O)--NH--(CH.sub.2).sub.a--R.sub.10, and the others are hydrogen, --OH or --OSO.sub.3, or (for R.sub.2)--OR.sub.12; and further provided that at least one and not more than four of R.sub.2--R.sub.9 are --OH or --OSO.sub.3; and pharmaceutically acceptable salts and esters thereof are active against a broad spectrum of microorganisms, and may therefore be used in the treatment of microbial infections.

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First Claim