Antituberculosis agent-10
Antituberculosis agent-10 (Compound 9) has excellent antibacterial activity against Mycobacterium tuberculosis (MIC = 0.3 μM). Antituberculosis agent-10 inhibits protein synthesis by targeting the 50S ribosomal subunit of the bacterium, thus exerting its antibacterial effect. Antituberculosis agent-10 is orally active.
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- CAS. Nr.: 2095636-19-2
- Formel: C17H17FN2O4S
- Molecular Weight:364.39
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Biologische Aktivität
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Biologische Aktivität
Beschreibung
In Vitro
Antituberculosis agent-10 (72 h) is inactive in inhibiting mitochondrial protein synthesis (MPS) in HepG2 cells (IC50 = 150 μM), but its metabolites shows mitochondrial toxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Antituberculosis agent-10 ((i.g.; 4 mg/kg; twice daily for one week then once daily ) reduces the volume of tuberculosis foci in Mtb-infected marmosets with potent antibacterial activity[1].
Pharmacokinetic Analysis in Antituberculosis agent-10[1]
| Route | Dose (mpk) | Cl/Clu (mL/min/kg) | Vd/Vdu (L/kg) | MRT/ss t1/2 (h) | F (%) |
| i.v. | 2 | 12/316 | 0.6/16 | 0.8/0.6 | / |
| p.o. | 10 | / | / | / | 64 |