| 摘要 |
The invention relates to 3-amino-methyl derivatives of rifamycin SV having the general formula <FORM:1090115/C2/1> wherein B is <FORM:1090115/C2/2> or <FORM:1090115/C2/3> wherein R is H or C1- 8 alkyl, hydroxy C1- 8 alkyl, carboxy C1- 8 alkyl o cycloalkyl, X is methylene, ethylene, -CH2O- or -CH2NH- and R11 and R111 each represent H, C1- 8 alkyl, OH or carboxy; and the N-oxides of said compounds. The compounds are produced by treating rifamycin S with formaldehyde and a compound of formula HB, wherein B is as defined above, and contacting the obtained aminomethyl derivative of rifamycin S with an aqueous solution of ascorbic acid to reduce the quinone system to the hydroquinone system of the desired rifamycin SV derivative. The N-oxides are obtained by treating the 3-amino-methyl derivative of rifamycin SV with aqueous hydrogen peroxide. Therapeutic compositions comprise the above 3-aminomethyl derivatives of rifamycin SV or their N-oxides and a carrier. They have broad spectrum antibacterial activity and may be used orally. |
