1029280-03-2Relevant academic research and scientific papers
R-3-Amino-1-((3aS,7aS)-octahydro-1H-indol-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-one derivatives as potent inhibitors of dipeptidyl peptidase-4: Design, synthesis, biological evaluation, and molecular modeling
Wang, Sinan,Su, Mingbo,Wang, Jiang,Li, Zeng,Zhang, Lei,Ji, Xun,Li, Jingya,Li, Jia,Liu, Hong
, p. 6684 - 6693 (2015/02/19)
A series of (R)-3-amino-1-((3aS,7aS)-octahydro-1H-indol-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-one derivatives was designed, synthesized, and evaluated as novel inhibitors of dipeptidyl peptidase-4 (DPP-4) for the treatment of type 2 diabetes. Most of the synthesized compounds demonstrated good inhibition activities against DPP-4. Among these, compounds 3e, 4c, 4l, and 4n exhibited prominent inhibition activities against DPP-4, with IC50s of 0.07, 0.07, 0.14, and 0.17 μM, respectively. The possible binding modes of compounds 3e and 4n with dipeptidyl peptidase-4 were also explored by molecular docking simulation. These potent DPP-4 inhibitors were optimized for the absorption, distribution, metabolism, and excretion (ADME) properties, and compound 4n displayed an attractive pharmacokinetic profile (F = 96.3%, t1/2 = 10.5 h).
Synthesis of new perhydroindole derivatives and their evaluation in ruthenium-catalyzed hydrogen transfer reduction
Liegault, Benoit,Tang, Xiaoping,Bruneau, Christian,Renaud, Jean-Luc
experimental part, p. 934 - 940 (2009/04/05)
New perhydroindole derivatives were synthesized with good yields and evaluated as chiral ligands in the RuII-catalyzed hydride transfer reduction of acetophenone. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
