13807-89-1Relevant articles and documents
Enzyme-Mediated Directional Transport of a Small-Molecule Walker with Chemically Identical Feet
Martin, Christopher J.,Lee, Alan T. L.,Adams, Ralph W.,Leigh, David A.
, p. 11998 - 112002 (2017)
We describe a small-molecule "walker" that uses enzyme catalysis to discriminate between the relative positions of its "feet" on a track and thereby move with net directionality. The bipedal walker has identical carboxylic acid feet, and "steps" along an isotactic hydroxyl-group-derivatized polyether track by the formation/breakage of ester linkages. Lipase AS catalyzes the selective hydrolysis of the rear foot of macrocyclized walkers (an information ratchet mechanism), the rear foot producing an (R)-stereocenter at its point of attachment to the track. If the hydrolyzed foot reattaches to the track in front of the bound foot it forms an (S)-stereocenter, which is resistant to enzymatic hydrolysis. Only macrocyclic walker-track conjugates are efficiently hydrolyzed by the enzyme, leading to high processivity of the walker movement along the track. Conventional chemical reagents promote formation of the ester bonds between the walker and the track. Iterative macrocyclization and hydrolysis reactions lead to 68% of walkers taking two steps directionally along a three-foothold track.
NUCLEOSIDE PRODRUGS AND USES RELATED THERETO
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Page/Page column 207; 208, (2021/02/26)
Disclosed are acyclic nucleoside prodrugs with improved metabolic stability and oral bioavailability. In general, the prodrugs are derivatives of acyclic nucleoside phosphonates containing a lipid-like moiety that can increase oral absorption and subsequent stability in the liver and plasma. Preferably, the lipid-like moiety can resist enzyme-mediated ω-oxidation, such as ω -oxidation catalyzed by cytochrome P450 enzymes. Also disclosed are pharmaceutical formulations of the acyclic nucleoside prodrugs. The acyclic nucleoside prodrugs and pharmaceutical formulations thereof can be used to treat viral infections, such as HIV infections, and/or viral-associated cancer, such as HPV-associated cancers.
Compound as well as preparation method and medical application thereof
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Paragraph 0252-0255, (2020/02/14)
The invention provides a compound as well as a preparation method and medical application thereof, the compound has a structure as shown in a general formula (I), and can also be a tautomer, a mesomer, a raceme, an enantiomer, a diastereoisomer, or a mixture form thereof, or a pharmaceutically acceptable salt thereof. According to the compound with the structure as shown in the general formula (I)provided by the invention, a specific main chain structure and a corresponding substituent group are selected, so that the obtained compound can be used as an arginase inhibitor, is relatively high in activity, and has a potential treatment prospect in various diseases.