Results 11 to 20 of about 957 (147)

Investigation of Isobactin Analogues of Teixobactin [PDF]

ACS Medicinal Chemistry Letters
Although teixobactin is a promising antibiotic drug candidate against Gram-positive bacteria, it aggregates to form gels that may limit intravenous administration. We previously reported O-acyl isopeptide prodrugs of teixobactin analogues that address the problem of gel formation while retaining antibiotic activity. We termed these compounds isobactins.
Chelsea R Jones, Grant H Lai, James S Nowick   +2 more
exaly   +7 more sources

New Teixobactin Analogues with a Total Lactam Ring [PDF]

ACS Medicinal Chemistry Letters, 2023
Teixobactin is a new antibiotic peptide with strong efficacy against several Gram-positive resistant bacteria, the structure of which is extremely difficult to obtain in the laboratory via multistep conventional synthesis. To face the increasing antibiotic resistant bacteria, it is fundamental to introduce new types of antibiotics with innovative ...
Marta Bauer, Wojciech Kamysz, Anish Parmar   +2 more
exaly   +7 more sources

Total synthesis of teixobactin [PDF]

Nature Communications, 2016
Teixobactin is a recently identified antibiotic that shows activity against drug resistant strains of bacteria. Here, the authors report a highly convergent total synthesis of this natural product, with sufficient flexibility to also allow the synthesis ...
Kang Jin, Iek Hou Sam, Kathy Hiu Laam Po, Du’an Lin, Ebrahim H. Ghazvini Zadeh, Sheng Chen, Yu Yuan, Xuechen Li   +7 more
doaj   +13 more sources

Isobactins: O-acyl isopeptide prodrugs of teixobactin and teixobactin derivatives. [PDF]

Chem Sci, 2022
O-Acyl isopeptide prodrug analogues of the antibiotic teixobactin are stable and non-gelating at acidic pH but convert to the corresponding active teixobactin analogues at neutral pH, thus overcoming limitations in intravenous dosing of teixobactin.
Jones CR, Guaglianone G, Lai GH, Nowick JS.   +3 more
europepmc   +7 more sources

A Fluorescent Teixobactin Analogue [PDF]

ACS Chemical Biology, 2020
This report describes the first synthesis and application of a fluorescent teixobactin analogue that exhibits antibiotic activity and binds to the cell walls of Gram-positive bacteria. The teixobactin analogue, Lys(Rhod)9,Arg10-teixobactin, has a fluorescent tag at position 9 and an arginine in place of the natural allo-enduracididine residue at ...
Michael A. Morris, Melody Malek, Mohammad H. Hashemian, Betty T. Nguyen, Sylvie Manuse, Kim Lewis, James S. Nowick   +6 more
core   +6 more sources

Elucidation of the Teixobactin Pharmacophore [PDF]

ACS Chemical Biology, 2016
This paper elucidates the teixobactin pharmacophore by comparing the arginine analogue of teixobactin Arg10-teixobactin to seven homologues with varying structure and stereochemistry. The roles of the guanidinium group at position 10, the stereochemistry of the macrolactone ring, and the "tail" comprising residues 1-5 are investigated.
Yang, Hyunjun, Chen, Kevin, Nowick, James   +2 more
openaire   +6 more sources

Synthesis and application of fluorescent teixobactin analogs [PDF]

, 2022
Teixobactin is a promising new antibiotic that kills a spectrum of Gram-positive pathogens that are considered to be urgent threats by the CDC and the WHO. Better understanding of the novel mechanism of action of teixobactin may assist in developing new antibiotics and furthering our understanding of antibiotic resistance.
Morris, Michael A, Jones, Chelsea R, Nowick, James S   +2 more
openaire   +5 more sources

X-ray crystallographic structure of a teixobactin analogue reveals key interactions of the teixobactin pharmacophore [PDF]

Chemical Communications, 2017
X-ray crystallography reveals key interactions in the pharmacophore of the antibiotic teixobactin.
H. Yang, D. R. Du Bois, J. W. Ziller, J. S. Nowick   +3 more
openaire   +6 more sources

Teixobactin kills bacteria by a two-pronged attack on the cell envelope [PDF]

Nature, 2022
Antibiotics that use novel mechanisms are needed to combat antimicrobial resistance(1–3). Teixobactin(4) represents a new class of antibiotics with a unique chemical scaffold and lack of detectable resistance. Teixobactin targets lipid II, a precursor of
Rhythm Shukla, Maik G N Derks, Chelsea R Jones   +2 more
exaly   +4 more sources

Teixobactin Provides Protection against Inhalation Anthrax in the Rabbit Model

Pathogens, 2020
The use of antibiotics is a vital means of treating infections caused by the bacteria Bacillus (B.) anthracis. Importantly, with the potential future use of multidrug-resistant strains of B.
William S. Lawrence, Jennifer E. Peel, Satheesh K. Sivasubramani, Wallace B. Baze, Elbert B. Whorton, David W. C. Beasley, Jason E. Comer, Dallas E. Hughes, Losee L. Ling, Johnny W. Peterson   +9 more
doaj   +2 more sources