Koester, Dennis C. et al. published their research in Journal of Medicinal Chemistry in 2022 | CAS: 109-85-3

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Many esters have the potential for conformational isomerism, but they tend to adopt an s-cis (or Z) conformation rather than the s-trans (or E) alternative, due to a combination of hyperconjugation and dipole minimization effects. The preference for the Z conformation is influenced by the nature of the substituents and solvent, if present. Lactones with small rings are restricted to the s-trans (i.e. E) conformation due to their cyclic structure.Category: ethers-buliding-blocks

Discovery of quinoline-based proteasome inhibitors for human African trypanosomiasis (HAT) was written by Koester, Dennis C.;Marx, Vanessa M.;Williams, Sarah;Jiricek, Jan;Dauphinais, Maxime;Rene, Olivier;Miller, Sarah L.;Zhang, Lei;Patra, Debjani;Chen, Yen-Liang;Cheung, Harry;Gable, Jonathan;Lakshminarayana, Suresh B.;Osborne, Colin;Galarneau, Jean-Rene;Kulkarni, Upendra;Richmond, Wendy;Bretz, Angela;Xiao, Linda;Supek, Frantisek;Wiesmann, Christian;Honnappa, Srinivas;Be, Celine;Maser, Pascal;Kaiser, Marcel;Ritchie, Ryan;Barrett, Michael P.;Diagana, Thierry T.;Sarko, Christopher;Rao, Srinivasa P. S.. And the article was included in Journal of Medicinal Chemistry in 2022.Category: ethers-buliding-blocks The following contents are mentioned in the article:

Human African Trypanosomiasis (HAT) is a vector-borne disease caused by kinetoplastid parasites of the Trypanosoma genus. The disease proceeds in two stages, with a hemolymphatic blood stage and a meningo-encephalic brain stage. In the latter stage, the parasite causes irreversible damage to the brain leading to sleep cycle disruption and is fatal if untreated. An orally bioavailable treatment is highly desirable. A brain-penetrant, parasite-selective 20S proteasome inhibitor that was rapidly optimized from an HTS singleton hit to drug candidate, I [wherein, X = C, N; R1 = Me, chloro, bromo; R2 = 2-fluoro, 2,3-difluoro, 2,6-difluoro; R3 = cyclopropyl, (2R)-2-fluoro-3-hydroxy-Pr, (2R)-3-hydroxy-2-methoxy-propyl; R4 = H; R3R4 = C4H8], among them I [wherein, X = C, R1 = chloro, R2 = 2,3-difluoro, R3 = (2R)-3-hydroxy-2-methoxy-propyl; R4 = H] that showed cure in a stage II mouse efficacy model was reported. Hit expansion and lead optimization campaign guided by cryo-electron microscopy and an in-silico model to predict the brain-to-plasma partition coefficient Kp as an important parameter to prioritize compounds for synthesis was described. The model combined with in-vitro and in-vivo experiments allowed us to advance compounds with favorable unbound brain-to-plasma ratios (Kp,uu) to cure a CNS disease such as HAT. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Category: ethers-buliding-blocks).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Many esters have the potential for conformational isomerism, but they tend to adopt an s-cis (or Z) conformation rather than the s-trans (or E) alternative, due to a combination of hyperconjugation and dipole minimization effects. The preference for the Z conformation is influenced by the nature of the substituents and solvent, if present. Lactones with small rings are restricted to the s-trans (i.e. E) conformation due to their cyclic structure.Category: ethers-buliding-blocks

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem