3-Amidino ansamycins

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Bacterium or component thereof or substance produced by said...

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42424854, 424258, 424244, 2602393P, A61K 31395, C07D49808

Patent

active

043270964

ABSTRACT:
Novel 3-amidino rifamycins having the formula: ##STR1## wherein Y is --H or --COCH.sub.3 ; R.sub.1 and R.sub.2 may be linear or branched alkyl having from 1 to 7 carbon atoms and alkenyl having 3 or 4 atoms and R.sub.2 may be also chloroalkyl having from 2 to 4 carbon atoms, cycloalkyl having from 3 to 7 carbon atoms in the ring, cycloalkylalkyl having from 3 to 6 carbon atoms in the ring, phenyl, bornyl, arylalkyl hydrocarbon having 7 or 8 carbon atoms which may be substituted with one halogen atom in the aryl group; and R.sub.1 and R.sub.2 along with the N atom to which they are bonded form an unsubstituted cyclic moiety having from 5 to 8 carbon atoms, a cyclic moiety having from 5 to 8 carbon atoms substituted with 1 or 2 methyl radicals, 4-alkylpiperazine, morpholine, 1,2,3,4-tetrahydroisoquinoline.
These novel compounds are from grey to dark solids having high antibacterial activity which are obtained by reacting 3-amino rifamycin S or SV with a chloroformiminio chloride.

REFERENCES:
patent: 4124585 (1978-11-01), Mars et al.

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