Substituted derivative of phosphorus oxyacids, use thereof and pharmaceutical composition containing it
Abstract
The present invention relates to a antituberculosis active substances based on phosphorus oxyacid derivatives with substituted salicylanilides of the general formula I, in which Re1, Re2 = a hydrogen atom, a halogen atom or NOi2; Re3, Re4 = a hydrogen atom, a halogen atom or NOi2, or CFi3; Re5 = H, halogen, or NOi2; Re6 = alkyl containing 2 to 16 carbon atoms, aryl having 6 to 18 carbon atoms, aryloxy containing 6 to 18 carbon atoms, or arylalkyloxy having 6 to 18 carbon atoms in the aryl moiety and 2 to 16 carbon atoms in the alkyloxy moiety; Re7 = aryl containing 6 to 18 carbon atoms, aryloxy having 6 to 18 carbon atoms, arylalkyloxy having 6 to 18 carbon atoms in the aryl moiety and 2 to 16 carbon atoms in the alkyloxy moiety or it is omitted; Re8 = a hydrogen atom or a dingle bond to phosphorus. These compounds, which can be prepared by simple syntheses, exhibit high activity against mycobacteria including multiresistant strains thereof.
The invention also discloses the use of that type of phosphorus oxyacid aromatic derivatives and salicylanilides of the general formula I as antituberculosis agents and/or antimycobacterial medicaments. Further, the invention also discloses a pharmaceutical composition in which the derivative of the general formula I is comprised as an active substance.