ABSTRACT
A number of semisynthetic rifamycin derivatives modified at position 3 and/or 4, belonging to general structures 2 and 4 (see Scheme 1), have been obtained. The synthesis and the biological activities of the new compounds are described. Compounds 4p and 4q display very good antimycobacterial activity in mice.
Subject(s)
Rifamycins/chemical synthesis , Animals , Bacteria/drug effects , Female , Indicators and Reagents , Magnetic Resonance Spectroscopy , Mice , Microbial Sensitivity Tests , Mycobacterium tuberculosis/drug effects , Rifampin/toxicity , Rifamycins/toxicity , Structure-Activity RelationshipABSTRACT
A number of semisynthetic rifamycin derivatives, modified at position 3, belonging to general structures (II), (III), (IV), (V), (VI), (VII) and (VIII) (see Scheme), have been prepared. The synthesis, structure, and antimicrobial evaluation of the new compounds are described. All the derivatives have in vitro antibacterial activities comparable with that of rifampicin.
Subject(s)
Bacteria/drug effects , Rifamycins/chemical synthesis , Chemical Phenomena , Chemistry , Magnetic Resonance Spectroscopy , Microbial Sensitivity Tests , Mycobacterium tuberculosis/drug effects , Rifamycins/pharmacologyABSTRACT
A number of semisynthetic rifamycin derivatives modified at positions 3 and/or 4, belonging to general structures 3, 5, and 6 (see Scheme 1), have been prepared. The synthesis, structure and antimicrobial evaluation of the new compounds are described. All the derivatives have "in vitro" antibacterial activities well comparable with that of rifampicin.
