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Hitchings, Elion, Vanderwerff, and Falco (1) demonstrated that certain 2,4-diamino-pyrimidines inhibited the growth of L. casei; this inhibition could be reversed by folic acid and citrovorum factor. The effects of these active pyrimidines are activity is associated with the presence of 2 and 4 amino groups in the pyriniidine nucleus, and a weighty substituent in the 5 position, suggesting a definite similarity in molecular configuration to the folic acid antagonists (Figure FIGURE 1 N AMINOPTERIN Cl NH2 1/ Cl' HN S N CH: 2,4-diamino-5-(3',4'-dichlorophenyl)-6-methylpyrimidine (DDMP)
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Murphy et al. (1954) studied this question.
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