CYCLIC DEPSYPEPTIDE DERIVATIVES HAVING 18 RING ATOMS, OPTICAL ISOMERS AND RACEMATES THEREOF, USE THEREOF AS AGENT FOR CONTROLLING ENDOPARASITES, AND ENDOPARASITICIDAL AGENT

摘要

FIELD: microbiology. SUBSTANCE: cyclic depsypeptide derivatives of general formula (I): wherein R₁ is linear of branched alkyl having 2-8 carbon atoms, hydroxyalkyl, alkanoyloxyalkyl, alkoxyalkyl, aryloxyalkyl, marcaptoalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, carboxyalkyl, alkoxycarbonylalkyl, arylalkoxycarbonylalkyl, carbamoylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, quanidinoalkyl unsubstituted or substituted by one or two benzyloxycabonyl residues or 1- 4 alkyl radicals, alkoxycarbonylaminoalkyl, 9- fluoroenylmethoxycarbonyl aminoalkyl, alkenyl, cycloalkyl, cycloalkylalkyl and also unsubstituted or substituted arylalkyl, the substituents being halogen, hydroxyl, alkyl and alkoxy R₂ wherein R₄ are independently from each other linear or branched alkyl having 1 to 8 carbon atoms, hydroxyalkyl, alkanoyloxyalkyl, alkoxyalkyl, aryloxyalkyl, mercaptoalkyl, alkylthioalkyl, alkylsulfinylalkyl, arylsulfonylalkyl, carboxyalkyl, alkoxycarbonylalkyl, arylalkoxycarbonylalkyl, carbamoylalkyl, aminoalkyl, alkylaminoalky, dialkylaminoalkyl, quanidinoalkyl unsubstituted or substituted by one or two benzyloxycarbonyl radicals or 1-4 alkyl radical; alkoxycarbonylaminoalkyl, 9- fluoroenylmethoxycarbonylaminoalkyl, alkenyl, cycloalkyl, cycloalkylalkyl and also unsubstituted or substituted aralkyl, the substituents being halogen, alkyl and alkoxy; R₃ and R₅ are independently of each other linear and branched alkyl having from 1 to 8 carbon atoms, hydroxyalkyl, alkanoyloxyalkyl, alkoxyalkyl, aryloxyalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, carboxyalkyl, alkoxycarbonylalkyl, arylalkoxycarbonylalkyl, carbamoyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonylaminoalkyl, alkenyl, cycloalkyl, cycloalkylalkyl and also unsubstituted or substituted aryl and aralkyl, the substituents being halogen, hydroxyl, alkyl and alkoxyl, or optical isomers or racemates thereof. Claimed invention also describes use of cyclic depsypeptide derivatives of general formula of (II): wherein R₆,R₈ and R₁₀ are independently from each other linear or branched alkyl having 1 to 8 carbon atoms, hydroxyalkyl, alkanoyloxyalkyl, alkoxyalkyl, aryloxyalkyl, mercaptoalkyl, alkylthioalkyl, alkylsulfinylalkyl, arylsulfonylalkyl, carboxyalkyl, alkoxycarbonylalkyl, arylalkoxycarbonyalkyl, carbamoylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, guanidinoalkyl unsubstituted or substituted by one or two benzyloxycarbonyl radicals or 1-4 alkyl radicals; alkoxycarbonylaminoalkyl, 9- fluoroenylmethoxycarbonylaminoalkyl, alkenyl, cycloalkyl, cycloalkylalkyl and also unsubstituted or substituted arylalkyl, the substituents being halogen, alkyl and alkoxy; R₇,R₉ and R₁₁ are independently of each other linear and branched alkyl having from 1 to 11 carbon atoms, hydrxyalkyl, alkanoyloxyalkyl, alkoxyalkyl, aryloxyalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, carboxyalkyl, alkoxycarbonylalkyl, arylalkoxycarbonylalkyl, carboamoylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonylaminoalkyl, alkenyl, cycloalkyl, cycloalkylalkyl and also unsubstituted or substituted aryl and arylalkyl, the substituents being halogen, hydroxyl, alkyl and alkoxyl, or optical isomers or racemates thereof as agent for controlling endoparasites. Claimed invention also describes endoparasiticidal agent containing active ingredient and at least one physiologically tolerant carrier, the active ingredient comprising compound of formula (I) and (II) given above, or optical isomer or racemate thereof in effective amount. EFFECT: improved properties of the title compounds.