Fabimycin

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Fabimycin
Names
IUPAC name
(E)-3-(7-amino-8-oxo-5,6,7,9-tetrahydropyrido[2,3-b]azepin-3-yl)-N-methyl-N-[(3-methyl-1-benzofuran-2-yl)methyl]prop-2-enamide
Identifiers
3D model (
JSmol
)
  • InChI=1S/C23H24N4O3/c1-14-17-5-3-4-6-19(17)30-20(14)13-27(2)21(28)10-7-15-11-16-8-9-18(24)23(29)26-22(16)25-12-15/h3-7,10-12,18H,8-9,13,24H2,1-2H3,(H,25,26,29)/b10-7+
    Key: ZWQNEFFHBSGFHV-JXMROGBWSA-N
  • CN(CC1=C(C)C2=CC=CC=C2O1)C(=O)\C=C\C1=CC2=C(NC(=O)C(N)CC2)N=C1
Properties
C23H24N4O3
Molar mass 404.470 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).

Fabimycin is an newly developed antibiotic candidate which is effective against gram-negative bacterias, an unusually problematic class of bacteria that uses thicker cell walls and molecular efflux pumps to protect themselves by preventing the antibiotics reaching inside the cells.[1][2]

Antibiotic resistance

Main article:
Antibiotic resistance

Global deaths attributable to antimicrobial resistance (AMR) numbered 1.27 million in 2019. That year, AMR may have contributed to 5 million deaths and one in five people who died due to AMR were children under five years old.[3] The European Centre for Disease Prevention and Control calculated that in 2015 there were 671,689 infections in the EU and European Economic Area caused by antibiotic-resistant bacteria, resulting in 33,110 deaths. Most were acquired in healthcare settings.[4]

History

Researchers modified the structure of Debio-1452,[5] an under-development antibiotic that is active against gram positive bacteria, and its derivative, which is moderately effective against non-resistant gram-negative bacteria.[1][6] The drug inhibits the bacterial enzyme FabI, which is an important enzyme in bacterial fatty acid biosynthesis. Clinical trials targeting the enzyme for use in S. aureus (Gram +ve) infections have reached Phase 2 inhibitors.[2]

Fabimycin was tested in mice against more than 200 colonies of resistant bacteria, across 54 strains of

urinary tract infections, pushing bacteria levels lower than before infection in mouse models.[1]

Further, it did not affect some types of

gut microbiome.[1]

See also

References

  1. ^ a b c d Irving, Michael (2022-08-11). "New antibiotic molecule kills dozens of the toughest types of superbugs". New Atlas. Retrieved 2022-08-11.
  2. ^
    PMID 36032774
    .
  3. S2CID 246077406
    .
  4. ^ "Antibiotic-resistant bacteria responsible for over 33,000 deaths in Europe in 2015, study finds". Pharmaceutical Journal. 7 November 2018. Archived from the original on 7 October 2019. Retrieved 16 December 2018.
  5. PMID 25691627
    .
  6. ^ Davis, Joe (2022-08-11). "Antibiotic-resistant bacteria: New drug can fight off 300 different types of superbugs". timetotimes.com. Retrieved 2022-08-11.

attribution This page contains text copyrighted with a CC-BY-4.0 license from European Centre for Disease Prevention and Control

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