2, 4-Diamino-5-benzylpyrimidines and analogs as antibacterial agents. 5. 3', 5'-Dimethoxy-4'-substituted-benzyl analogs of trimethoprim

B Roth, E Aig, BS Rauckman, JZ Strelitz…

文献索引：Roth; Aig; Rauckman; Strelitz; Phillips; Ferone; Bushby; Sigel Journal of Medicinal Chemistry, 1981 , vol. 24, # 8 p. 933 - 941

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被引用次数: 41

摘要

Forty trimethoprim analogues in which the para substituent in the benzene ring was varied were prepared for antibacterial evaluation. All were very potent inhibitors of Escherichia coli dihydrofolate reductase. The similarity of their inhibitory activities strongly suggested that the side chains beyond the fiist two atoms were not in contact with the enzyme. However, among 38 ether derivatives which varied widely in their bulk and lipophilicity, very few ...