Antimycotic peptide-amino-ether derivs. - esp. active against Candida species are tetra:hydro-SL 7810/F-II, S 31794/F-I, aculeacine A and tetra:hydro-equinocandine B derivs.

摘要

Peptidic-amino-ethers of formula (I) and their acid addn. salts (when n = 0) are novel cpds. In (I), n = 0 and (a) A is 2-8C alkylene; R1 is such that R1OH is tetrahydro-SL 7810/F-II or S31794/F-I or aculeacine A; R2 is H, 1-12C alkyl, 3-6C alkenyl or alkynyl in which the multiple bond is not in the alpha-position w.r.t. to N atom to which the gp. is joined, 3-7C cycloalkyl, 3-7C cycloalkyl-1-4C alkyl, 2-hydroxyethyl, 3-hydroxypropyl, 3-6C 2-alkoxyethyl, furylmethyl, tetrahydrofurylmethyl, thienylmethyl, pyridylmethyl; etc., 4-piperidinyl, 1-(1-4C alkyl)-4-piperidinyl, phenyl or 7-11C phenalkyl (in which the benzene rings are opt. substd. by 1 or 2 gps. independently chosen from F, Cl, Br, hydroxy, 1-4C alkyl and 1-4C alkoxy; R3 is H, 1-6C alkyl, 2-hydroxyethyl, 3-hydroxypropyl or 3-6C 2-alkoxyethyl or R2 and R3 together are -CH2-CH2-B-CH2-CH2- where B is a bond, -CH2- or -O-; (b) A is 2-8C branched chain alkylene; R1 is such that R1OH is tetrahydro-SL 7810/F-II or S3 1794/F-I, aculeacine A or tetrahydro-equinocandine B and R2, R3 independently are H, methyl or ethyl; or (c) A is 2-8C straight chain alkylene; R1 is such that R1OH is tetrahydro-equinocandine B; R2 is 3-6C alkenyl or alkynyl in which the multiple bond is not in the alpha-position w.r.t. the N-atom to which the gp. is joined and R3 is H, 1-6C alkyl, 2-hydroxyethyl, 3-hydroxypropyl or 3-6C 2-alkoxyethyl or (d) A is 2-8C (branched) alkylene; R1 is such that R1OH is tetrahydro-SL-7810/F-II, aculeacine A or tetrahydroequinocandine B and R2 is -C(NHR6)=N-R5 (Gp. II); R5, R6 each are H or 1-6C alkyl or together are ethylene or -(CH2)3- and R3 is H; or n is 1 and A is 2-6C (branched) alkylene; R1 is such that R1OH is tetrahydro-SL 7810/F-II, aculeacine A or tetrahydro-equinocandine B; R2 is 1-4C alkyl, allyl, 2-propynyl or benzyl; R3 is 1-4C alkyl or R2 and R3 together are -(CH2)4- or -(CH2)5-; R4 is (m)ethyl and X circled negative is an anion. With the condition that when A is branched alkylene and n=1 then R2 and R3 each are (m)ethyl. (I) are antimycotics having excellent activity against yeasts and lower fungi partic. against strains of Candida, pathogenic to man.