Novel polycyclic hydrazones of rifamycins, their manufacture, and their pharmaceutical compositions for treating tuberculosis

摘要

Novel hydrazones derived from 3-formylrifamycin S or SV as the aldehydo component and a bi- or tri-cyclic N-aminopiperazine as the hydrazino component and having the formula (I) in which R1, R2, R3, R4, R5 and R6, independently of one another, each represents a hydrogen atom or C1-4-alkyl, m and n, independently of one another, each represents an integer from 0 to 5, X represents C1-5-alkylidene, benzylidene or C1-4-alkoxymethylene, Y represents C1-5-alkylidene, C1-4-alkoxymethylene, oxy, thio or optionally substituted imino of the formula -N(R)- wherein R represents hydrogen, C1-4-alkyl, C3-5-alkenyl, C3-12-cycloalkyl or phenyl, or X and Y together represent 1,2-cycloalkylene or o-phenylene each of which can be substituted by from one to three C1-4-alkyl radicals, and Rif represents a radical of rifamycin S or SV that is bonded in the 3-position by the free valency, are distinguished by a high and long-lasting antituberculotic activity. They are manufactured in conventional manner, for example by condensation of their components.