| 摘要 |
<p>PURPOSE:To obtain the new derivative of specific formula, useful as an antifungal agent, an anti-inflammatory agent, etc., and having an inhibitory action on acidic protease of Candida albicans. CONSTITUTION:This derivative is expressed by formula I (R<1> and R<2> are H or carboxyl or a 1-10C alkoxycarbonyl which may be interrupted with one to three oxygen atoms; R<3> is H or lower alkyl; R<4> and R<7> are lower alkyl; R<5> is a 4-8C cycloalkyl of ring skeleton; R<6> is a lower alkyl which may be replaced with hydroxy group), e.g. (2S,4S,5S)-N-butyl-6-cyclohexyl-4-hydroxy-2- isopropyl-5-[N(alpha)-(4-methoxycarbonylbenzoyl)-L-norleucylamino] hexanamide. The derivative is obtained, for example, by deprotecting an amine of formula II (Pa is amine-protecting group), reacting the amine with a carboxlic acid to give a peptide, deprotecting the peptide, then reacting the resultant substance with a carboxylic acid derivative of formula III and aminating the reaction product.</p> |
