Isoflavonoid antibacterial compounds, compositions and use

Details Isoflavonoid antibacterial compounds, compositions and use Isoflavonoid antibacterial compounds, compositions and use

1993-11-24

1995-03-21

Ramsuer, Robert W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514253, 514468, 544 79, 544357, 546256, 546270, 549214, 549383, A61K 3135, A61K 31535, C07D49304

Patent

active

053995589

ABSTRACT:
Methods, compounds and compositions are provided for inhibiting the growth of mycobacteria and gram-positive organisms in vitro and of treatment of mycobacterial and gram-positive infections in vivo using compounds of the formula (I) or (II): ##STR1## wherein R.sub.1 is hydrogen, halogen, amino or loweralkyl; and R.sub.2 is selected from the group consisting of --CONR.sub.4 R.sub.5, --(CH.sub.2).sub.n- NR.sub.4 R.sub.5, --NHCO--NR.sub.4 R.sub.5 and --NHCO.sub.2 R.sub.4, wherein R.sub.4 and R.sub.5 are selected from hydrogen, loweralkyl, alkoxy, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, arylalkylaryl, arylaryl, aryoxy, aryloxyaryl, aryloxyarylalkyl, arylalkoxy, arylalkoxyaryl, arylalkoxyarylalkyl, arylalkoxyaryl, alkenyl, alkynyl and heterocycle, or R.sub.4 and R.sub.5 are connected to form a ring and produce cycloalkyl or heterocycle; and n is 0, 1, 2, or 3; or a pharmaceutically acceptable salt thereof processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and a method of treating disorders resulting from mycobacterial or MRSA infections. The methods, compounds and compositions are particularly useful for inhibiting the growth of Mycobacterium tuberculosis, and may be used alone, or in combination with other anti-Mycobacterium tuberculosis agents, such as isoniazid, rifampin, pyrazinamide, rifabutin, streptomycin and ciprofioxacin, to provide new agents for the treatment of tuberculosis, including multidrug-resistant tuberculosis (MDRTB).

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