New 5-substd. 2,4-di:amino-pyrimidine cpds. - are antibacterial and antimycotic agents, esp. active against tuberculosis bacteria and Candida albicans

摘要

2,4-diaminopyrimidine derivs. of formula (I) are new, where X = O, S or CH2, R = phenyl or naphthyl opt. substd. by halogen, Me, Et, OMe or OEt. USE/ADVANTAGE - (I) are antimycobacterial and antimycotic agnets, e.g. with higher activity than trimethoprim against mycobacterium tuberculosis and other mycobacterium spp. and against Candida albicans dihydrofolate reductase (DHFR). Synergistic effects may be administered by combinations of (I) with dihydrofolate synthase inhibitors such as sulphonamides or 4,4'-diaminodiphenyl sulphone. In an example a mixt. of 480mg 2,4-diamino-5-hydroxypyrrimidine 2HCl, 650 mg 1-naphthylmethyl chloride and 9ml 2-methoxymethanol pretreated with 170 mg Na was stirred at room temp. for 4 days, treated with 50ml of 3N NaOH, and the ppte. filtered off and recrystd. from MeOH to give 2,4-diamino-5- (1-naphthylmethoxy) -pyrimidine (Ia), m.pt. 190 deg.C.