Quality Control of 2-Aminopropane-1,3-diolIn 2021 ,《Design, synthesis, and structure-activity relationship of programmed cell death-1/programmed cell death-ligand 1 interaction inhibitors bearing a benzo[d]isothiazole scaffold》 appeared in European Journal of Medicinal Chemistry. The author of the article were Chen, Hao; Wang, Ke; Yang, Yang; Huang, Xupeng; Dai, Xinyan; Feng, Zhiqiang. The article conveys some information:
A novel series of compounds such as I [R = CH2NHCHCO2HCH2OH, CH2(N-piperidin-3-ol), CH2(N-pyrrolidin-3-ol), etc.] bearing a benzo[d]isothiazole scaffold were developed, among which compound I [R = CH2NHCHCO2HCH2OH] exhibited promising activity, with an IC50 value of 8.5 nM. Further cell-based PD-1/PD-L1 blockade bioassays indicated that compound I [R = CH2NHCHCO2HCH2OH] could inhibit the PD-1/PD-L1 interaction at the cellular level, with an EC50 value of 5.6μM compound I [R = CH2NHCHCO2HCH2OH] could had better potency in restoring the activity of effector cells, as the maximal luminescence values (RLUmax) of compound I [R = CH2NHCHCO2HCH2OH] were equivalent to those of PD-L1 mAbs. The docking anal. of compound I [R = CH2NHCHCO2HCH2OH] with the PD-L1 dimer complex (PDB ID: 6R3K) confirmed that I [R = CH2NHCHCO2HCH2OH] was a promising lead compound for the development of inhibitors of the PD-1/PD-L1 interaction. The preliminary structure-activity relationship was investigated in this paper, with the aim of future drug development. After reading the article, we found that the author used 2-Aminopropane-1,3-diol(cas: 534-03-2Quality Control of 2-Aminopropane-1,3-diol)
2-Aminopropane-1,3-diol(cas: 534-03-2) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).Quality Control of 2-Aminopropane-1,3-diol
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