The article 《LAT1 activity of carboxylic acid bioisosteres: Evaluation of hydroxamic acids as substrates》 also mentions many details about this compound(10466-61-2)Application In Synthesis of H-Leu-NH2.HCl, you can pay attention to it or contacet with the author([email protected]; [email protected]) to get more information.
Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 10466-61-2, is researched, SMILESS is N[C@@H](CC(C)C)C(N)=O.[H]Cl, Molecular C6H15ClN2OJournal, Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov’t, Bioorganic & Medicinal Chemistry Letters called LAT1 activity of carboxylic acid bioisosteres: Evaluation of hydroxamic acids as substrates, Author is Zur, Arik A.; Chien, Huan-Chieh; Augustyn, Evan; Flint, Andrew; Heeren, Nathan; Finke, Karissa; Hernandez, Christopher; Hansen, Logan; Miller, Sydney; Lin, Lawrence; Giacomini, Kathleen M.; Colas, Claire; Schlessinger, Avner; Thomas, Allen A., the main research direction is LAT1 carboxylic acid bioisostere hydroxamate; Acyl sulfonamide; Amino acid; SLC7A5; Tetrazole; Transporter inhibitor; Transporter substrate.Application In Synthesis of H-Leu-NH2.HCl.
Large neutral amino acid transporter 1 (LAT1) is a solute carrier protein located primarily in the blood-brain barrier (BBB) that offers the potential to deliver drugs to the brain. It is also up-regulated in cancer cells, as part of a tumor’s increased metabolic demands. Previously, amino acid prodrugs have been shown to be transported by LAT1. Carboxylic acid bioisosteres may afford prodrugs with an altered physicochem. and pharmacokinetic profile than those derived from natural amino acids, allowing for higher brain or tumor levels of drug and/or lower toxicity. The effect of replacing phenylalanine’s carboxylic acid with a tetrazole, acylsulfonamide and hydroxamic acid (HA) bioisostere was examined Compounds were tested for their ability to be LAT1 substrates using both cis-inhibition and trans-stimulation cell assays. As HA-Phe demonstrated weak substrate activity, its structure-activity relationship (SAR) was further explored by synthesis and testing of HA derivatives of other LAT1 amino acid substrates (i.e., Tyr, Leu, Ile, and Met). The potential for a false pos. in the trans-stimulation assay caused by parent amino acid was evaluated by conducting compound stability experiments for both HA-Leu and the corresponding Me ester derivative The authors concluded that HA’s are transported by LAT1. In addition, the results lend support to a recent account that amino acid esters are LAT1 substrates, and that hydrogen bonding may be as important as charge for interaction with the transporter binding site.
The article 《LAT1 activity of carboxylic acid bioisosteres: Evaluation of hydroxamic acids as substrates》 also mentions many details about this compound(10466-61-2)Application In Synthesis of H-Leu-NH2.HCl, you can pay attention to it or contacet with the author([email protected]; [email protected]) to get more information.
Reference:
Chiral Catalysts,
Chiral catalysts – SlideShare