Teixobactin

Names

[ Name ]:
Teixobactin

[Synonym ]:
(R)-N1-((2R,3S)-1-(((2S,3S)-1-(((S)-1-(((3S,6S,9S,12R,13S)-3-((S)-sec-butyl)-6-(((S)-2-iminoimidazolidin-4-yl)methyl)-9,13-dimethyl-2,5,8,11-tetraoxo-1-oxa-4,7,10-triazacyclotridecan-12-yl)amino)-3-hydroxy-1-oxopropan-2-yl)amino)-3-methyl-1-oxopentan-2-yl)amino)-3-methyl-1-oxopentan-2-yl)-2-((S)-3-hydroxy-2-((2S,3S)-3-methyl-2-((R)-2-(methylamino)-3-phenylpropanamido)pentanamido)propanamido)pentanediamide

Biological Activity

[Description]:

Teixobactin is a potent antibiotic. Teixobactin shows antibacterial activity for gram-negative bacteria. Teixobactin inhibits cell wall synthesis by binding to a highly conserved motif of lipid II and lipid III[1][2][3].

[Related Catalog]:

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Bacterial

[In Vitro]

Teixobactin (0-128 µg/mL) 显示出抗菌活性，对 MRSA ATCC 33591 的 MIC 值为 0.25 µg/mL[2]。 Teixobactin (0-24 h) 显示出抗菌活性，对 Clostridium difficile, Bacillus anthracis 的 MIC 值分别为5、20 ng/mL[3]。

[In Vivo]

Teixobactin (1-20 mg/kg; i.v.; once) 在小鼠体内表现出抗菌活性[3]。 Animal Model: Female CD-1 mice (MRSA ATCC33591)[3] Dosage: 1, 2.5, 5, 10, 20 mg/kg Administration: i.v.; once; one hour post-infection Result: Showed good antibacterial activity and all treated animals survived.

[References]

[1]. Piddock LJ. Teixobactin, the first of a new class of antibiotics discovered by iChip technology? J Antimicrob Chemother. 2015 Oct;70(10):2679-80.

[2]. Parmar A, et al. Teixobactin analogues reveal enduracididine to be non-essential for highly potent antibacterial activity and lipid II binding. Chem Sci. 2017 Dec 1;8(12):8183-8192.

[3]. Ling LL, et al. A new antibiotic kills pathogens without detectable resistance. Nature. 2015 Jan 22;517(7535):455-9.

Chemical & Physical Properties

[ Molecular Formula ]:
C₅₈H₉₅N₁₅O₁₅

[ Molecular Weight ]:
1242.47000

[ Exact Mass ]:
1241.71000

[ PSA ]:
460.79000

[ LogP ]:
1.52230

Related Compounds

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