DNA gyrase inhibitors and pharmaceutical preparations therefor

Compounds of the formula ##STR65## in which X.sup.1 is --S-- or --SO--;

• X.sup.2 is --CO-- or --CS--;
• R.sup.1 is hydrogen, halogen or lower alkyl optionally substituted by halogen or lower alkoxy;
• R.sup.2 and R.sup.3 are each independently selected from hydrogen, lower alkyl, halogen, amino, lower alkylamino, dilower alkylamino, acylamino, lower alkoxy, lower alkoxymethoxy and a group OR.sup.4 ;
• R.sup.4 is hydrogen or an easily hydrolyzable group;
• R.sup.5 is hydrogen, optionally esterified carboxy or amidated (thio)-carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted acyl or heterocyclyl;
• R.sup.6 and R.sup.7a are each independently hydrogen or lower alkyl;
• R.sup.7b is hydrogen, optionally substituted hydroxy, --NR--A or --N.dbd.B, in which R is hydrogen or lower alkyl, A is hydrogen, optionally substituted alkyl, lower cycloalkyl, iminoyl, (thio)acyl, esterified carboxy or amidated (thio)carboxy and B is lower alkylidene;
• or
• R.sup.7a and R.sup.7b together represent oxo, lower alkoxycarbonylmethylidene or optionally substituted hydroxyimino;
• and
• R.sup.8 is hydrogen, optionally substituted alkyl, optionally esterified carboxy or amidated (thio)carboxyl;
• provided that no more than two of R.sup.1 -R.sup.3 are nitrogen-containing groups;
• no more than two of R.sup.1 -R.sup.3 are oxygen containing groups and no more than two of R.sup.1 -R.sup.3 are either nitrogen containing or oxygen containing groups;
• and R.sup.20, R.sup.30 and R.sup.70b are as R.sup.2, R.sup.3 and R.sup.7b respectively above except that at least one of these substituents represents nitro.

A pharmaceutical preparation comprising a therapeutically effective amount of a compound having the formula ##STR66## wherein X.sup.1 is --S-- or --SO--;

• X.sup.2 is --CO-- or --CS--;
• R.sup.1 is hydrogen, halogen or lower alkyl optionally substituted by halogen or lower alkoxy;
• R.sup.2 and R.sup.3 are each independently selected from hydrogen, lower alkyl, halogen, amino, lower alkylamino, dilower alkylamino, acylamino, lower alkoxy, lower alkoxymethoxy and a group OR.sup.4 ;
• R.sup.4 is hydrogen or an easily hydrolyzable group;
• R.sup.5 is hydrogen, optionally esterified carboxy or amidated (thio)-carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted acyl or heterocyclyl;
• R.sup.6 and R.sup.7a are each independently hydrogen or lower alkyl;
• R.sup.7b is hydrogen, optionally substituted hydroxy, --NR--A or --N.dbd.B, in which R is hydrogen or lower alkyl, A is hydrogen, optionally substituted alkyl, lower cycloalkyl, iminoyl, (thio)acyl, esterified carboxy or amidated (thio)carboxy and B is lower alkylidene;
• or
• R.sup.7a and R.sup.7b together represent oxo, lower alkoxycarbonylmethylidene or optionally substituted hydroxyimino;
• and
• R.sup.8 is hydrogen, optionally substituted alkyl, optionally esterified carboxy or amidated (thio)carboxy;
• provided that no more than two of R.sup.1 -R.sup.3 are nitrogen-containing groups;
• no more than two of R.sup.1 -R.sup.3 are oxygen containing groups and no more than two of R.sup.1 -R.sup.3 are either nitrogen containing or oxygen containing groups;
• and a therapeutically inert carrier.