38792-42-6Relevant articles and documents
BIM-46174 fragments as potential ligands of G proteins
Küppers, Jim,Benkel, Tobias,Annala, Suvi,Schnakenburg, Gregor,Kostenis, Evi,Gütschow, Michael
, p. 1838 - 1843 (2019)
The 5,6,7,8-Tetrahydroimidazo[1,2-A]pyrazine derivative BIM-46174 has received attention as Gαq inhibitor. We conducted structural reductions to monocyclic and bicyclic substructures to explore the chemical space of BIM fragments and to gain insights into the pharmacophore of BIM-Type Gαq inhibitors. Two piperazin-2-one-containing fragments and a small library of bicyclic lactams featuring fused pyrazine and diazepine rings were synthesized and evaluated. The results of a second messenger-based cellular assay indicate that the entire BIM structure is required for efficient Gαq inhibition.
Asymmetric synthesis of optically active methyl-2-benzamido-methyl-3-hydroxy-butyrate by robust short-chain alcohol dehydrogenases from Burkholderia gladioli
Chen, Xiang,Liu, Zhi-Qiang,Huang, Jian-Feng,Lin, Chao-Ping,Zheng, Yu-Guo
supporting information, p. 12328 - 12331 (2015/07/27)
Three short-chain alcohol dehydrogenases from Burkholderia gladioli were discovered for their great potential in the dynamic kinetic asymmetric transformation of methyl 2-benzamido-methyl-3-oxobutanoate, and their screening against varied organic solvents and substrates. This is the first report of recombinant enzymes capable of achieving this reaction with the highest enantio- and diastereo-selectivity.
3-(Hydroxy(phenyl)methyl)azetidin-2-ones obtained via catalytic asymmetric hydrogenation or by biotransformation
Rimoldi, Isabella,Cesarotti, Edoardo,Zerla, Daniele,Molinari, Francesco,Albanese, Domenico,Castellano, Carlo,Gandolfi, Raffaella
scheme or table, p. 597 - 602 (2011/06/21)
The catalytic asymmetric reduction of ethyl-2-(benzamidomethyl)-3-oxo- phenylpropanoate was realized with high enantiomeric and diastereoisomeric excesses via biotransformation using whole cells of different yeasts and asymmetric hydrogenation with Ru(II)