1609670-80-5
Chemical Structure
TXA709
- CAS No.: 1609670-80-5
- Formula:C22H19F5N4O3S
- Molecular Weight:514.47
InChIKey: LOTYKTRNFDRNAY-UHFFFAOYSA-N
SMILES: O=C(C1=C(F)C(OCC2=NC3=C(S2)N=CC(C(F)(F)F)=C3)=CC=C1F)NC(C4CCN(CC4)C)=O
Biological Activity: TXA709 is an orally active FtsZ-targeting prodrug that hydrolyzes to the active metabolite TXA707 (HY-153695). TXA709 inhibits bacterial (bacterial) Z-ring cytokinesis by targeting FtsZ, exerts bactericidal activity against Staphylococcus aureus isolates including Vancomycin (HY-B0671)-, Daptomycin (HY-B0108)-, and Linezolid (HY-10394)-resistant strains, and shows synergistic effects when combined with Cefdinir (HY-B0136) or Oxacillin (HY-B0925A). TXA709 can be used for research on MRSA infections and Staphylococcus aureus infections[1][2][3][4][5].
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TXA709 | TXA709 is an orally active FtsZ-targeting prodrug that hydrolyzes to the active metabolite TXA707 (HY-153695). TXA709 inhibits bacterial (bacterial) Z-ring cytokinesis by targeting FtsZ, exerts bactericidal activity against Staphylococcus aureus isolates including Vancomycin (HY-B0671)-, Daptomycin (HY-B0108)-, and Linezolid (HY-10394)-resistant strains, and shows synergistic effects when combined with Cefdinir (HY-B0136) or Oxacillin (HY-B0925A). TXA709 can be used for research on MRSA infections and Staphylococcus aureus infections. | |||||||||||||||||||||
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References
- [1]. Kaul M, et al. TXA709, an FtsZ-Targeting Benzamide Prodrug with Improved Pharmacokinetics and Enhanced In Vivo Efficacy against Methicillin-Resistant Staphylococcus aureus. Antimicrob Agents Chemother. 2015 Aug;59(8):4845-55. [Content Brief]
- [2]. Kaul M, et al. Combining the FtsZ-Targeting Prodrug TXA709 and the Cephalosporin Cefdinir Confers Synergy and Reduces the Frequency of Resistance in Methicillin-Resistant Staphylococcus aureus. Antimicrob Agents Chemother. 2016 Jun 20;60(7):4290-6.
- [3]. Lepak AJ, et al. In Vivo Pharmacodynamic Evaluation of an FtsZ Inhibitor, TXA-709, and Its Active Metabolite, TXA-707, in a Murine Neutropenic Thigh Infection Model. Antimicrob Agents Chemother. 2015 Oct;59(10):6568-74. [Content Brief]
- [4]. Kaul M, et al. Combination with a FtsZ inhibitor potentiates the in vivo efficacy of oxacillin against methicillin-resistant Staphylococcus aureus. Med Chem Res. 2022 Oct;31(10):1705-1715. [Content Brief]
- [5]. Bi F, et al. Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators. European journal of medicinal chemistry. 2018 Nov 05;159:90-103. [Content Brief]
