30100-16-4Relevant articles and documents
Mechanically induced gelation of a kinetically trapped supramolecular polymer
Teunissen, Abraham J. P.,Nieuwenhuizen, Marko M. L.,Rodrguez-Llansola, Fransico,Palmans, Anja R. A.,Meijer
, p. 8429 - 8436 (2014)
The stimuli-induced gelation of a urethane-functionalized ditopic ureidopyrimidinone (UPy) compound is presented, and the mechanism by which the gelation proceeds is proposed. In a 40-120 mM solution in chloroform, the compound can exist in two different aggregated states, namely a low viscous mixture of (cyclic) oligomers or a fibrous gel. As evidenced by IR, NMR, and WAXS, the liquid state is stabilized by hydrogen bonds between the UPy and the back-folded chain, while the fibrous gel is stabilized by lateral hydrogen bonds within stacked UPy dimers. Controlled preparation techniques allow for pathway selection to arrive at one of both states. The remarkable long-term stability of the low viscous state (over 2 months for a 80 mM solution) is in contrast to the fast transformation into a gel by stirring in a few hours. Other mechanical stimuli like shaking, sonicating, and stirring for a shorter period, as well as freezing and thawing the solution, yield weaker gels than those obtained by long stirring. Heating the gels and slow cooling reversibly yield the nonviscous solution. This shows that the formation of UPy-urethane hydrogen bonds kinetically traps the UPy polymers, thereby preventing their lateral aggregation. The application of mechanical stress or freezing disrupts this interaction, allowing for the formation of a stacked nucleus on which further material can grow, eventually leading to gelation of the solution.
A practical synthesis of ω-aminoalkanoic acid derivatives from cycloalkanones
Ho, Koc-Kan,O'Toole, Doris C.,Achan, Douglas M.,Lim, Kitae T.,Press, Jeffery B.,Leone-Bay, Andrea
, p. 2641 - 2649 (1996)
A practical synthetic route to N-Boc protected or Boc-amino acid coupled ω-aminoalkanoic acids is reported and exemplified by the preparation of 8-(t-butoxycarbonylamino)caprylic acid 2 and (N-t-butoxycarbonylphenylalanyl)-8-aminocaprylic acid 3. The sequence does not involve column chromatography, hydrogenation, azide or bromide related rearrangements, and therefore is amenable to scale-up. Homologues of the ω-aminoalkanoic acid derivatives may also be prepared by using different cycloalkanones.
Design, synthesis and activity study of a novel PI3K degradation by hijacking VHL E3 ubiquitin ligase
Li, Chuchu,Liu, Xiaoqing,Ma, Mingliang,Wang, Haili
, (2022/03/31)
PI3K kinase plays an important role in regulating key processes in cells, such as cell growth, metabolism, proliferation, and apoptosis. The overexpression of PI3K kinase exists in many cancers. The proteolytic target chimera (PROTAC) technology is a new technology that uses the ubiquitin–proteasome system to degrade a given target protein. It has been described that CRBN-based PROTAC targets the degradation of PI3K kinase. However, PROTAC based on VHL has not been reported yet. Here, we connected the previously obtained highly active PI3K inhibitor to the VHL ligand through different small molecules, and obtained a series of PROTAC molecules targeting PI3K kinase. Obtain the most active compound through screening. It provides evidence for the feasibility of PROTAC technology to recruit VHL E3 ligase in PI3K kinase.
MACROCYCLIC COMPOUNDS USEFUL AS CHITINASE INHIBITORS
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Paragraph 0131; 0134-0135, (2021/07/29)
The present invention relates to macrocyclic compounds of formula (I) and their use as chitinase inhibitors as well as to pharmaceutical compositions and methods of preparation thereof. The compounds can in particular be used in the treatment, prevention and/or amelioration of asthma.
GLYCOPEPTIDE COMPOUNDS, METHODS FOR PRODUCING THE SAME, AND USES THEREOF
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Paragraph 0158; 0160, (2020/12/14)
Disclosed herein are novel compounds and uses thereof. The present compounds are useful in suppressing the growth of various bacteria, including gram-positive and gram-negative bacteria. Accordingly, these compounds may be used to manufacture a medicament or pharmaceutic composition for treating disease and/or disorders associated with bacterial infection, especially antibiotic-resistant bacterial infection. Al so disclosed herein are methods for treating infectious diseases by use of the present compounds, medicament or pharmaceutical composition.
