Inhibitor of dihydrofolate reductase

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Bacterium or component thereof or substance produced by said...

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26023975, 260465E, 544325, A61K 31505, C07D23949, C07D23949

Patent

active

042580455

ABSTRACT:
A group of aryl-Z-alkoxy-5-benzylpyrimidines wherein Z is oxy, thio, imino, carbonyl, carbamoyl, sulfonyl, sulfinyl or sulfamoyl has been prepared from 2,4-diamino-5-benzylpyrimidine via alkylation with either an aryl-Z-alkyl halide or a substituted glycidyl ether. These compounds are potent dihydrofolate reductase (DHFR) inhibitors which are useful as antibacterial, anti-protozoal and antitumor agents.

REFERENCES:
patent: 2909522 (1959-10-01), Hitchings et al.
patent: 3049544 (1962-08-01), Stenbuck et al.
patent: 3692787 (1972-09-01), Roth et al.
patent: 3931181 (1976-01-01), Kompis et al.
patent: 3992379 (1976-11-01), Liebenow et al.
Lednicer et al., The Organic Chemistry of Drug Synthesis, pp. 120 to 123, John Wiley & Sons, NY, (1977).

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