Chemistry of carbon compounds – Miscellaneous organic carbon compounds – C-metal
Patent
1980-09-30
1982-10-12
Bond, Robert T.
Chemistry of carbon compounds
Miscellaneous organic carbon compounds
C-metal
424244, 424267, 424250, 42424854, 424246, C07D52100
Patent
active
043538266
ABSTRACT:
Antibiotically active compounds derived from rifamycin S or from the corresponding hydroquinone, rifamycin SV, or from derivatives at least partially hydrogenated in positions 16, 17; 18, 19; 28, 29, such as the 16, 17; 18, 19--tetrahydro- or the 16, 17; 18, 19; 28, 29--hexahydro derivatives, which contain in position 3 a free or an aliphatically substituted amino group. The hydrocarbon radicals of the aliphatically substituted amino group can also be interrupted in their carbon chain by heteroatoms and/or be substituted by functional groups.
A special group of these new compounds is represented by 3-amino derivatives as defined above, in which the amino group is a particular type of N-aza-cyclo-aliphatic radical unsubstituted by functional groups, and which has, in addition to the antibiotic action against sensitive microorganisms also an antibacterial activity against certain types of resistant microorganisms.
Another special group is represented by 3-amino derivatives as defined above, in which the amino group is a particular type of a 4R-1-piperazinyl radical, in which R is a hydrocarbon radical; they have a special high antituberculosis action, while having very low toxicity.
REFERENCES:
patent: 3542765 (1970-11-01), Bickel et al.
patent: 4005077 (1977-01-01), Bickel et al.
patent: 4261891 (1981-04-01), Bickel et al.
Fieser, "J. Am. Chem. Soc.", vol. 48 (1926), pp. 2922-2937.
Beilstein, "Handbuch der Organischen Chemie", Band 14, pp. 162-163 (1931).
Bernthsen and Sudborough, "Organic Chemistry", 4th Ed. (Blackie) (1941), pp. 499-500.
Bickel Hans
Kump Wilhelm
Almaula Prabodh I.
Bond Robert T.
Ciba-Geigy Corporation
Glynn Michael W.
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