PEPTIDE DERIVATIVE, ITS PHARMACOLOGICALLY PERMISSIBLE SALT, ITS PRODUCTION AND USE

摘要

PROBLEM TO BE SOLVED: To provide a new compound selectively inhibiting the proteolytic activity of Arg-gingipain and useful as a preventive and treating agent for periodontosis. SOLUTION: The objective compound is expressed by formula I [X is CHOH or CO; A<1> and A<2> are each lysyl, or histidyl; R<1> is H or nitro; R<2> is a substituted oxycarbonyl; R<3> is OR<4> or NR<5> R<6> (R<4> to R<6> are each a lower alkyl)], e.g. the compound of formula II. The objective compound can be produced by treating a peptide derivative of formula III (A<3> and A<4> are each a protected lysyl derivative or a protected histidyl derivative; R<7> is H, nitro or a protecting group) and its pharmacologically permissible salt with a dilute acid (e.g. hydrochloric acid) in a proper solvent (e.g. chloroform) or in the absence of solvent and subjecting the treated product to deprotecting reaction by using anisole, etc., as a reaction acceleration agent.