2,4-Di:amino-methoxy-5-benzyl-pyrimidine derivs. - bacteriostatic agents useful for treatment of staphylococcus infections and to potentiate sulphamide(s)

摘要

derivs. of formula (I) and their acid addn. salts are new. In (I) one of X1 and X2 = methoxy and the other is alkyl, aryloxy or halo. Also claimed are compsns. contg. (I) and a sulphamide. (I) are bacteriostatic agents, active against gram-positive and gram-negative bacteria and partic. useful for the treatment of staphylococcus infections. They also potentiate the activity of sulphamides, such as sulphamethoxazole, sulphalene, sulphadimethoxine, sulphadiazine, sulphaquinoxaline, sulphafurazole and sulphacetamide, e.g. (I) (X1 = Cl, X2 = CH3O) synergistic compsns. with sulphamethoxazole allow reduced quantities of sulphamethoxazole to be used than when trimethoprim is used, as potentiator. (I) may be administered orally (5-500 mg doses), rectally (200-400 mg) or parenterally (50-200 mg). The cpds. have low-toxicity e.g. 2g/Kg LD50. MIC are given and compared with trimethoprim. Pref. (I) has (a) X1 = methoxy and X2 - methyl, isopropyl, phenoxy, chloro or fluoro and (b) X2 = methoxy and X1 = methyl, isopropyl, phenoxy and chloro.