Month: May 2024

Levell, Julian R. et al. published their research in ACS Medicinal Chemistry Letters in 2017 | CAS: 99395-88-7

(S)-4-Phenyloxazolidin-2-one (cas: 99395-88-7) belongs to oxazolidine derivatives.Oxazolidines are readily available also from propargyl amines. In another report, the incorporation of an additional substituted oxazolidine ring over a range of new biphenylazepinium salt organocatalysts for the asymmetric epoxidation of alkenes improved enantiocontrol over the parent structures.Formula: C9H9NO2

Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1 was written by Levell, Julian R.;Caferro, Thomas;Chenail, Gregg;Dix, Ina;Dooley, Julia;Firestone, Brant;Fortin, Pascal D.;Giraldes, John;Gould, Ty;Growney, Joseph D.;Jones, Michael D.;Kulathila, Raviraj;Lin, Fallon;Liu, Gang;Mueller, Arne;van der Plas, Simon;Slocum, Kelly;Smith, Troy;Terranova, Remi;Toure, B. Barry;Tyagi, Viraj;Wagner, Trixie;Xie, Xiaoling;Xu, Ming;Yang, Fan S.;Zhou, Liping X.;Pagliarini, Raymond;Cho, Young Shin. And the article was included in ACS Medicinal Chemistry Letters in 2017.Formula: C9H9NO2 This article mentions the following:

High throughput screening and subsequent hit validation identified 4-isopropyl-3-(2-((1-phenylethyl)amino)pyrimidin-4-yl)oxazolidin-2-one as a potent inhibitor of IDH1R132H. Synthesis of the four sep. stereomers identified the (S,S)-diastereomer (IDH125, 1f) as the most potent isomer. This also showed reasonable cellular activity and excellent selectivity vs. IDH1wt. Initial SAR exploration identified the key tolerances and potential for optimization. X-ray crystallog. identified a functionally relevant allosteric binding site amenable to inhibitors which can penetrate the blood-brain barrier, and aided rational optimization. Potency improvement and modulation of the physico-chem. properties identified (S,S)-oxazolidinone IDH889 (5x) with good exposure and 2-HG inhibitory activity in a mutant IDH1 xenograft mouse model. In the experiment, the researchers used many compounds, for example, (S)-4-Phenyloxazolidin-2-one (cas: 99395-88-7Formula: C9H9NO2).

(S)-4-Phenyloxazolidin-2-one (cas: 99395-88-7) belongs to oxazolidine derivatives.Oxazolidines are readily available also from propargyl amines. In another report, the incorporation of an additional substituted oxazolidine ring over a range of new biphenylazepinium salt organocatalysts for the asymmetric epoxidation of alkenes improved enantiocontrol over the parent structures.Formula: C9H9NO2

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem