4-Guanylazo-4-deoxyrifamycin SV derivatives

Details 4-Guanylazo-4-deoxyrifamycin SV derivatives 4-Guanylazo-4-deoxyrifamycin SV derivatives

1971-02-18

1976-09-07

Higel, Floyd D.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

260239R, 260999, 424226, A61K 31655, A61L 1300, C07C10704

Patent

active

039793761

ABSTRACT:
Antimicrobial substances of the rifamycin family corresponding to the formula ##SPC1##
Wherein R is a substituted lower alkyl radical of the formula --(CH.sub.2).sub.n --A wherein n is the number 2 or 3, A stands for a hydroxyl group or for an ##EQU1## group where R.sub.3 and R.sub.4 individually may be hydrogen, lower alkyl, lower alkylamino-lower alkyl, di-lower alkylamino-lower alkyl or cycloalkyl and together with the nitrogen atom to which they are attached a heterocyclic ring; R.sub.1 is hydrogen or taken with R it may represent a lower alkylene radical to complete with the nitrogen atoms to which they are attached a heterocyclic ring; R.sub.2 is hydrogen or, when the nitrogen atom to which it is attached is a part of a heterocyclic ring a lower alkyl group. The compounds are prepared by condensing 4-guanylazo-4-deoxyrifamycin SV with a substituted aliphatic amine derivative corresponding to the formula H.sub.2 N--(CH.sub.2).sub.n --A wherein n and A have the significance previously given. The compounds have antimicrobial activity and are useful as antibiotics.

REFERENCES:
patent: 2513996 (1950-07-01), Haury
Greco et al., Chemical Abstracts, vol. 57, pp. 12474-12475 (1962).
Sensi et al., Antibiot. Chemotherapy, vol. 12, pp. 488-494 (1962).
Theilheimer, "Synthetic Methods of Organic Chemistry", p. 250 (1960).
Maggi et al., Chemical Abstracts, vol. 70, p. 347, 57609e (1969).
Ciba Ltd., Chemical Abstracts, vol. 71, pp. 406 to 407, 500 14u (1969).

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