3-(SUBSTITUTED ETHYL)-RIFAMYCIN DERIVATIVES USEFUL AS ANTIMICROBIAL AGENTS
The present invention is directed to novel 3-(substituted ethyl) rifamycin derivatives, pharmaceutical compositions containing them and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes.
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Page/Page column 15
(2010/03/02)
CHEMICAL MODIFICATIONS OF THE ALIPHATIC BRIDGE IN ANSAMYCINS. SYNTHESIS AND ACTIVITY OF 18,19-DIHYDRORIFAMYCIN S
The selective hydrogenation of the C(18)=C(19) double bond in the antibacterial antibiotic rifamycin S, achieved by reaction with hydrazine at 40 deg C, leads to 18,19-dihydrorifamycin S.This compound is less active than rifamycin S in inhibiting the bacterial enzyme DNA-dependent RNA polymerase.
3-Dialkylaminomethyl derivatives of rifamycin S is provided by reacting rifamycin S with an iminium salt in an organic solvent. This compound is converted to 3-dialkylaminomethyl derivatives by virtue of ascorbic acid.
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(2008/06/13)
A FACILE PREPARATION OF RIFAMYCIN DERIVATIVES BY USE OF MANGANESE DIOXIDE
Rifamycin O, rifamycin S and rifamycin SV were prepared in good yields (88-94percent) by the oxidation and hydrolytic cleavage of rifamycin B in the presence of manganese dioxide.
Seong, Baik Lin,Han, Moon Hi
p. 627 - 628
(2007/10/02)
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