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Studies on antimalarials. I. Synthesis and antimalarial activities of some derivatives of 2,4-diamino-5-substituted amino pyrimidines and 2,4-diamino-6-methyl-5-substituted amino pyrimidines

Zhang, X.P.; Zhang, X.J.; Zheng, X.H.; Chen, L.; Dai, Z.R.

Yao Xue Xue Bao 15(12): 711-718

1980

ISSN/ISBN: 0513-4870
PMID: 7257796
Document Number: 162124
A series of 2,4-diamino-5 substituted amino pyrimidines and 2,4-diamino-6-methyl-5 substituted amino pyrimidines were synthesized and tested for antimalarial activity in a Plasmodium yoelii - Anopheles stephensi - mouse model. 12 compounds showed some degree of activity. The most effective compounds, as judged by the degree of protection against infection afforded to test mice, were 2,4-diamino-5-(3',4-dichloro-benzlidene amino)pyrimidine and 2,4-diamino-5-[(4'-bromo-benzyl)-N-nitroso-amino]pyrimidine administered orally at 10 mg/kg for 3 consecutive days.

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