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Synthesis of Novel 4,6-Di(substituted)amino-1,2-dihydro-1,3,5-triazine Derivatives as Topical Antiseptic Agents.

  作者 Maeda, Shirou;Kita, Toshiko;Meguro, Kanji;  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2009年52-3;  页码  597-600  
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[摘要]A series of novel 4,6-di(substituted)amino-1,2-dihydro-1,3,5-triazines I (R1 = Ph, PhCH2CH2, n-octyl, 4-MeOC6H4CH2, etc.; R2 = Et, n-Pr, n-Bu, n-octyl, n-decyl, etc.), designed to have ClogP of 5.1-7.5, was synthesized and evaluated for their antiseptic properties by MIC and MBC tests against Gram-pos. and Gram-neg. bacteria, including MRSA, VRE, and P. aeruginosa. Among these compds., 4-alkyl-6-aralkyl derivs. having ClogP of 6.6-7.1 and 4-alkyl-6-aryl or 4,6-dialkyl derivs. with ClogP of 6.0-6.4 showed pronounced antibacterial activities in both tests.

 
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