Antifungal antibiotic tetra-hydro-echinocandin-b ether derivs. - prepd. e.g. by condensation of tetra-hydro-echinocandin B with amino-alcohol cpds.

摘要

New tetrahydro-echinocandin B derivs. are of formula (I) and their acid addn. salts. In (I) m = O, 1, 2 3 or 4; R1 = H; 1-12C alkyl; 3-7C cycloalkyl; (3-7C cycloalkyl)-(1-3C alkyl) phenyl or 7-10C phenylalkyl opt. mono- or disubstd. in the phenyl ring by 1-4C alkyl, 1-4C alkoxy, F, Cl, Br or OH (substituents being identical if disubstd.); hydroxyethyl; 3-6C alkoxyethyl; furylmethyl; or tetrahydrofurylmethyl; R2 = H or 1-4C alkyl; or R1 + R2 = -(CH2)2-A-(CH2)2-(A=-CH2-, -O- or -NR4-; R4 = H or 1-4 C alkyl); and R3 = residue of formula (II) (where R5 is -(CH2)16CH3). (I) have antimycotic activity, with little or no antibacterial activity. They are active against both yeasts and hyphomycetes, and are useful in the treatment of topical and systemic mycoses.