In vitro activities against mycobacteria of two long-acting rifamycins, FCE22807 and CGP40/469A (SPA-S-565).

  title={In vitro activities against mycobacteria of two long-acting rifamycins, FCE22807 and CGP40/469A (SPA-S-565).},
  author={Jean M. Dickinson and Denis Anthony Mitchison},
  volume={71 2},

In vitro bactericidal and in vivo therapeutic activities of a new rifamycin derivative, KRM-1648, against Mycobacterium tuberculosis

Against experimental murine tuberculosis, KRM-1648 exhibited significant therapeutic effects, in terms of prolonged survival times for mice compared with those with rifampin treatment, even at lower doses, such as 1 and 3 mg/kg.

Activity of two long-acting rifamycins, rifapentine and FCE 22807, in experimental murine tuberculosis.

Chemotherapeutic efficacy of a newly synthesized benzoxazinorifamycin, KRM-1648, against Mycobacterium avium complex infection induced in mice

KRM-1648 was not efficacious in suppressing the progression of pulmonary lesions and the increase in bacterial loads at the sites of infection, including lungs and spleen, at the late phase of infections, which may imply some difficulty with chemotherapy for AIDS-associated MAC infection, even with KRM- 1648 treatment.

Concentration-Dependent Mycobacterium tuberculosis Killing and Prevention of Resistance by Rifampin

D doses of rifampin higher than those currently employed would optimize the effect of r ifampin, if patients could tolerate them, and the important properties may include the efficient entry of the rifamycin into M. tuberculosis.

Rifamycins e Obstacles and opportunities

This review of the state-ofthe-art regarding rifamycins suggests that it is quite possible to devise improved rIFamycin analogs, and improved activity against rifampin-resistant strains by some analogs promises that further work in this area, especially if the information from co-crystal structures with RNA polymerase is applied, should lead to even better analogs.

Development of an Antibiotic: Microbiology

This chapter deals with the antibacterial agent that is only one molecule among a series of compounds prepared by chemists before becoming a drug. Preselection is a crucial stage in the life of a new

In vitro antimycobacterial activities of newly synthesized benzoxazinorifamycins

K RM-1648 and KRM-1657 inhibited intracellular growth of M. tuberculosis, and their efficacies were much greater than that of RMP, and the other derivatives had similar levels of in vitro activity against these mycobacteria.

Bactericidal action of ofloxacin, sulbactam-ampicillin, rifampin, and isoniazid on logarithmic- and stationary-phase cultures of Mycobacterium tuberculosis

The bactericidal actions of ofloxacin and sulbactam-ampicillin, alone and in combination with rifampin and isoniazid, on exponential-phase and stationary-phase cultures of a drug-susceptible isolate



Experimental models to explain the high sterilizing activity of rifampin in the chemotherapy of tuberculosis.

The view that the special part of the bacterial population that is killed more rapidly by rifampin than by isoniazid during short-course chemotherapy consists of bacilli dormant much of the time but occasionally metabolising for short periods.

Laboratory evaluation of a new long-acting 3-azinomethylrifamycin FCE 22250.

In the experimental mice infection sustained by Mycobacterium tuberculosis H37Rv, FCE 22250 shows an efficacy 14 times higher than rifampicin and is still therapeutic when administered once every three weeks.

New long-acting 3-azinomethyl-rifamycins.

A number of basic 3-azinomethyl-rifamycins have been prepared. Their synthesis and antibacterial activity in vitro are reported, as well as the preliminary pharmacokinetic data. While the

Assay of rifampicin in serum

Two methods for the assay of rifampicin in serum are described, a conventional plate diffusion method and a chemical extraction followed by measurement of the inhibition of uptake of 14C-uridine by Staphylococcus aureus.