156642-19-2Relevant academic research and scientific papers
Tailoring the Physicochemical Properties of Antimicrobial Peptides onto a Thiazole-Based γ-Peptide Foldamer
Bonnel, Clément,Legrand, Baptiste,Simon, Matthieu,Clavié, Margaux,Masnou, Agnès,Jumas-Bilak, Estelle,Kang, Young Kee,Licznar-Fajardo, Patricia,Maillard, Ludovic T.,Masurier, Nicolas
, p. 9168 - 9180 (2020/10/19)
Antimicrobial peptides (AMPs) are amphipathic molecules displaying broad-spectrum bactericidal activity, providing opportunities to develop a new generation of antibiotics. However, their use is limited either by poor metabolic stability or by high hemolytic activity. We herein addressed the potential of thiazole-based γ-peptide oligomers named ATCs as tunable scaffolds to design polycationic AMP mimetics. Knowing the side chain distribution along the backbone, we rationally designed facially amphiphilic sequences with bactericidal effect in the micromolar range. Since no hemolytic activity was detected up to 100 μM, this class of compounds has shown the potential for therapeutic development.
MODIFIED PEPTIDES AND THEIR USE
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, (2020/05/13)
The invention relates to a compound of formula (A) wherein n is an integer from 1 to 6, and R1, R1', R2, R2', R3, R3' are cationic or hydrophobic residues.
Pyrimidine derivatives as IL-8 receptor antagonists
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Page 29, (2010/02/06)
Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula I In these compounds, Q is preferably unsubstituted and substituted heterocyclyl; U is usually hydrogen or fluorine; and V is preferably hydrogen, halogen, alkyl, —O—alkyl or —S-alkyl. A representative example is:
2,2'-bis(aminomethyl)-4,4'-bithiazole as a new Cu(II)-dependent DNA cleaving agent
Sasaki, Hideaki,Takanori, So-Ichi,Yamamoto, Keisuke,Nakamoto, Yasuyuki
, p. 1761 - 1764 (2007/10/03)
A simple and readily available DNA cleaving agent, 2,2'- bis(aminomethyl)-4,4'-bithiazole at 50 μM concentration showed a significant cleaving activity for plasmid DNA only in the presence of Cu(II) under physiological conditions without any reducing agents.
