Synthesis of novel 4,6-di(substituted)amino-1,2-dihydro-1,3,5-triazine derivatives as topical antiseptic agents.
A series of novel 4,6-di(substituted)amino-1,2-dihydro-1,3,5-triazine derivatives designed to have ClogP of 5.1-7.5 was synthesized and evaluated for their antiseptic properties by MIC and MBC tests against Gram-positive and Gram-negative bacteria, including MRSA, VRE, and P. aeruginosa. Among these compounds, 4-alkyl-6-aralkyl derivatives having ClogP of 6.6-7.1 and 4-alkyl-6-aryl or 4,6-dialkyl derivatives with ClogP of 6.0-6.4 showed pronounced antibacterial activities in both tests.
Maeda
Shirou
S
CT Laboratory, Hamari Chemicals, Ltd., 1-4-29 Kunijima, Higashiyodogawa-ku, Osaka 533-0024, Japan. shirou-maeda@hamari.co.jp
Kita
Toshiko
T
Meguro
Kanji
K
D000287:Administration, Topical; D000891:Anti-Infective Agents, Local / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D016983:Enterococcus / Q000187:drug effects; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D014227:Triazines / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D020713:Vancomycin Resistance
D000891:Anti-Infective Agents, Local; D014227:Triazines