Gepotidacin
Gepotidacin Basic information
- Product Name:
- Gepotidacin
- Synonyms:
-
- Gepotidacin
- Buagafuran
- GSK-2140944
- Gepotidacin (GSK2140944)
- 3H,8H-2a,5,8a-Triazaacenaphthylene-3,8-dione, 2-[[4-[[(3,4-dihydro-2H-pyrano[2,3-c]pyridin-6-yl)methyl]amino]-1-piperidinyl]methyl]-1,2-dihydro-, (2R)-
- (R)-2-((4-(((3,4-dihydro-2H-pyrano[2,3-c]pyridin-6-yl)methyl)amino)piperidin-1-yl)methyl)-1,2-dihydro-3H,8H-2a,5,8a-triazaacenaphthylene-3,8-dione
- (R)-2-((4-(((3,4-Dihydro-2H-pyrano[2,3-c]pyridin-6-yl)methyl)amino)piperidin-1-yl)methyl)-1,2-dihydro-3H,8H-2a,5,8a-triazaacenaphthylene-3,8-dione , Gepotidacin
- CAS:
- 1075236-89-3
- MF:
- C24H28N6O3
- MW:
- 448.52
- EINECS:
- 202-303-5
- Mol File:
- 1075236-89-3.mol
Gepotidacin Chemical Properties
- Boiling point:
- 661.9±65.0 °C(Predicted)
- Density
- 1.52±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 7.14 mg/mL (15.92 mM)
- form
- Solid
- pka
- 7.88±0.10(Predicted)
- color
- White to yellow
- InChIKey
- PZFAZQUREQIODZ-LJQANCHMSA-N
- SMILES
- C1N2C3=C(C=CC2=O)N=CC(=O)N3[C@@H]1CN1CCC(NCC2N=CC3OCCCC=3C=2)CC1
Gepotidacin Usage And Synthesis
Description
Gepotidacin (GSK2140944) is a triazaacenaphtylene developed by GSK and belongs to the class of Novel Bacterial Topoisomerase Inhibitors (NBTI). This new antibiotic is currently being investigated in three phase 3 clinical trials.
Uses
Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor.
Mechanism of action
Gepotidacin's primary mechanism of action involves inhibiting bacterial DNA replication, specifically targeting DNA gyrase (topoisomerase II) and topoisomerase IV. These enzymes are vital for bacterial processes such as replication, transcription, and cell division, as they regulate the topological state of DNA during these activities.
in vivo
GSK2140944 MICs are 0.125 to 0.5 mg/L against the six MRSA isolates. ELF penetration ratios range from 1.1 to 1.4. Observed maximal decreases are 1.1 to 3.1 log10 CFU in neutropenic mice. The mean fAUC/MIC ratios required for stasis and 1-log-unit decreases are 59.3 ± 34.6 and 148.4 ± 83.3, respectively.
References
[1] Farrell DJ, et al. In Vitro Activity of Gepotidacin (GSK2140944) against Neisseria gonorrhoeae. Antimicrob Agents Chemother. 2017 Feb 23;61(3). DOI:10.1128/AAC.02047-16
[2] Biedenbach DJ, et al. In Vitro Activity of Gepotidacin, a Novel Triazaacenaphthylene Bacterial Topoisomerase Inhibitor, against a Broad Spectrum of Bacterial Pathogens. Antimicrob Agents Chemother. 2016 Jan 4;60(3):1918-23. DOI:10.1128/AAC.02820-15
[3] O'Riordan W, et al. Efficacy, Safety, and Tolerability of Gepotidacin (GSK2140944) in the Treatment of Patients with Suspected or Confirmed Gram-Positive Acute Bacterial Skin and Skin Structure Infections. Antimicrob Agents Chemother. 2017 May 24;61(6). DOI:10.1128/AAC.02095-16
[4] So W, et al. Pharmacodynamic Profile of GSK2140944 against Methicillin-Resistant Staphylococcus aureus in a Murine Lung Infection Model. Antimicrob Agents Chemother. 2015 Aug;59(8):4956-61. DOI:10.1128/AAC.00625-15
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