Pharmaceuticals Rifamycin Sodium Salt For Antibacterial CAS 14897-39-3 CAS NO.14897-39-3

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Application:

Rifamycin SV is a broad-spectrum semisynthetic antimicrobial agent of the rifamycin group. It is used to study potential genes, such as rif15 and rif16, which may be involved in the conversion of rifamycin SV into rifamycin B. It is a potential treatment for traveler's diarrhea (TD), Clostridium difficile-associated disease (CDAD) and rheumatoid knee synovitis. It is used in electron spin resonance studies.



Biochem/physiol Action:

Rifamycin SV inhibits selective (E.coli,B.subtilis) bacterial DNA-dependent RNA polymerase by binding to the polymerase β-subunit, a mechanism similar to rifabutin. It acts as a selective cytochrome P450 3A4 inducer. It has limited oral absorption that is active against Gram-positive bacteria and is moderately active against gram-negative organisms.

Mechanism of action:

The antibacterial activity of rifamycins relies on the inhibition of bacterial DNA-dependent RNA synthesis.[5] This is due to the high affinity of rifamycins for the prokaryotic RNA polymerase. The selectivity of the rifamycins depends on the fact that they have a very poor affinity for the analogous mammalian enzyme. Crystal structure data of the antibiotic bound to RNA polymerase indicates that rifamycin blocks synthesis by causing strong steric clashes with the growing oligonucleotide ("steric-occlusion" mechanism).[6][7] If rifamycin binds the polymerase after the chain extension process has started, no inhibition is observed on the biosynthesis, consistent with a steric-occlusion mechanism. Single step high level resistance to the rifamycins occurs as the result of a single amino acid change in the bacterial DNA dependent RNA polymerase.