| 摘要 |
1484481 Compositions containing benzylpyrimidines F HOFFMANN-LA ROCHE & CO AG 11 Sept 1974 [12 Sept 1973] 39617/74 Heading A5B [Also in Division C2] An antibacterial composition contains a benzylpyrimidine of the formula: wherein R<SP>1</SP> and R<SP>2</SP> are (C 1 -C 3 ) alkyl or alkoxy, or (C 2 or C 3 ) alkenyl or alkenyloxy; Z is NO 2 , NH 2 , pyrrolo, pyrrolidino, piperidino, NHR<SP>4</SP>, -N(R<SP>4</SP>) 2 , -NHR<SP>5</SP>, -NR<SP>4</SP>R<SP>5</SP>, -NR<SP>4</SP>COOR<SP>4</SP>, -NHCOOR<SP>4</SP>, -NHCONHR<SP>3</SP>, -NHCSNHR<SP>3</SP>, -N 3 , -N=N-N(R<SP>4</SP>) 2 or -N(NO)R<SP>4</SP>, R<SP>3</SP> is H, (C 1 -C 3 ) alkyl or (C 2 -C 3 ) alkenyl and R<SP>5</SP> is acyl, and salts thereof; in association with a compatible pharmaceutical carrier. Compounds of the above formula inhibit bacterial dihydrofolate reductase and potentiate the antibacterial activity of sulphonamides with which they may be combined. Specified sulphonamides are sulphisoxazole, sulphadimethoxine, sulphamethoxazole, 4-sulphanilamido-5, 6-dimethoxy-pyrimidine, 2-sulphanilamido-4, 5- dimethyl-pyrimidine, sulphaquinoxaline, sulphadiazine sulphamonomethoxine and 2-sulphanilamido-4, 5-dimethylisoxazole. Other inhibitors for enzymes involved in the folic acid biosynthesis may also be incorporated in the compositions. They may be applied orally, rectally or parenterally. |
