134019-73-1Relevant articles and documents
Solid-phase synthesis of peptidosulfonamide containing peptides derived from Leu-enkephalin
De Bont, Dries B.A.,Dijkstra, Gerard D.H.,Den Hartog, Jack A.J.,Liskamp, Rob M.J.
, p. 3035 - 3040 (1996)
Using Boc or Fmoc-protected β-substituted aminoethanesulfonyl chlorides (2-substituted taurylchlorides) the solid-phase synthesis of dipeptidosulfonamides as well as peptidosulfonamide containing peptides derived from Leu-enkephalin is described. The binding activity of the peptidosulfonamide YGGFL derivatives is reported.
Helical Antimicrobial Sulfono-γ-AApeptides
Li, Yaqiong,Wu, Haifan,Teng, Peng,Bai, Ge,Lin, Xiaoyang,Zuo, Xiaobing,Cao, Chuanhai,Cai, Jianfeng
, p. 4802 - 4811 (2015)
Host-defense peptides (HDPs) such as magainin 2 have emerged as potential therapeutic agents combating antibiotic resistance. Inspired by their structures and mechanism of action, herein we report the first example of antimicrobial helical sulfono-γ-AApeptide foldamers. The lead molecule displays broad-spectrum and potent antimicrobial activity against multi-drug-resistant Gram-positive and Gram-negative bacterial pathogens. Time-kill studies and fluorescence microscopy suggest that sulfono-γ-AApeptides eradicate bacteria by taking a mode of action analogous to that of HDPs. Clear structure-function relationships exist in the studied sequences. Longer sequences, presumably adopting more-defined helical structures, are more potent than shorter ones. Interestingly, the sequence with less helical propensity in solution could be more selective than the stronger helix-forming sequences. Moreover, this class of antimicrobial agents are resistant to proteolytic degradation. These results may lead to the development of a new class of antimicrobial foldamers combating emerging antibiotic-resistant pathogens.
TETRAZINES FOR HIGH CLICK RELEASE SPEED AND YIELD
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Page/Page column 232; 235, (2021/01/22)
Disclosed herein are tetrazines substituted with groups that result in a high click conjugation yield and high click release yields. In some of several other aspects, the invention relates to combinations and kits comprising said tetrazines and a dienophile, preferably a trans-cyclooctene. In another aspect, the compounds, combinations, and kits are for use as a medicament.
C26-LINKED RAPAMYCIN ANALOGS AS MTOR INHIBITORS
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, (2019/11/21)
The present disclosure relates to mTOR inhibitors. Specifically, the embodiments are directed to compounds and compositions inhibiting mTOR, methods of treating diseases mediated by mTOR, and methods of synthesizing these compounds.