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

  title={Laboratory evaluation of a new long-acting 3-azinomethylrifamycin FCE 22250.},
  author={C Della Bruna and Domenico Ungheri and Geraldo Alberto Sebben and Aurora Sanfilippo},
  journal={The Journal of antibiotics},
  volume={38 6},
FCE 22250 (3-(N-piperidinomethylazino)methylrifamycin SV) is a member of the new class of 3-azinomethylrifamycins characterized by a long persistance in animals, a good oral absorption and a broad antibacterial spectrum including mycobacteria. 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. 
Comparative anti-gonococcal activity of S-565, a new rifamycin.
Activity of two long-acting rifamycins, rifapentine and FCE 22807, in experimental murine tuberculosis.
New experimental drugs for the treatment of tuberculosis.
  • F. Parenti
  • Biology, Medicine
    Reviews of infectious diseases
  • 1989
New rifamycins have been developed that are as active as rifampin against mycobacteria but that also offer the advantage of high and prolonged serum levels and thus have the potential for once-weekly administration.
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.
Activity in vitro of Rifabutin, FeE 22807, Rifapentine, and Rifampin against Mycobacterium microti and M. tuberculosis and Their Penetration into
None of the rlfamyclns were concentrated In macrophages, the MICs being higher In the macrophagesthan In vitro by a factor of 2·fold for rlfabutin, 6.7·foldFor rlfampin, 20· fold for FCE 22807, and 26·fold For rlfapentine.
Six new rifamycin derivatives-F22, having high bactericidal activity against stationary organisms and a long half-life, was considered likely to be the most effective sterilising drug.
New Drugs and Strategies for Chemotherapy of Tuberculosis
By and large, availability of several powerful drugs and, more importantly, the evolution of optimal regimens and proper application of specific antituberculosis chemotherapy with these drugs should be given credit for this success.


LM 427, a new spiropiperidylrifamycin: in vitro and in vivo studies.
The spiropiperidylrifamycin LM 427 displays a broad spectrum of potent antibacterial activity in vitro and in vivo and is particularly effective in the therapy of experimental tubercular infections of mice.
Novel rifamycins. IV. 3-Aminomethylazinomethylrifamycins, a new class of rifamycins, endowed with remarkable antibacterial activity.
The synthesis and the biological activities of the new compounds 1, endowed with favorable pharmacokinetic behavior, are described. In particular, compound 1a has been chosen for further
Antibacterial activity of DL 473, a new semisynthetic rifamycin derivative.
DL 473, a new semisynthetic rifamycin, was 2-10 times more active in vitro than rifampicin (RAMP) against several clinical isolates of Mycobacterium tuberculosis and only slightly less active than
In vitro susceptibility of Mycobacterium avium complex and Mycobacterium tuberculosis strains to a spiro-piperidyl rifamycin.
The in vitro activity of LM 427 was tested in vitro against strains of the Mycobacterium avium complex and strains of M. tuberculosis, and showed that all strains susceptible to rifampin were also susceptible to LM 427.
A simplified method of evaluating dose-effect experiments.
The method provides means for the rapid test of parallelism of two curves and easy computation of relative potency with its confidence limits and its accuracy is commensurate with the nature of dose-per cent effect data.
Rifampicin, a general review.
SANFILIPPO: LM 427, a new spiropiperidyl rifamycin: In vitro and in vivo studies
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  • 1983
SANFILIPPO: Attivita delle ansamicine LM 427 e FCE 22250 su micobatteri atipici in vitro
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KILBURN: In vitro susceptibility of M. aviunt complex and M. tuberculosis strains to a spiro-piperidyl-rifamycin
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WILCOxoN: A simplified method of evaluating dose response experiments
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