id author title date pages extension mime words sentences flesch summary cache txt cord-321858-c5m4dj9m Yoshizawa, Shin-ichiro Evaluation of an octahydroisochromene scaffold used as a novel SARS 3CL protease inhibitor 2020-02-15 .txt text/plain 6519 337 56 The inhibitory activities of the diastereoisomerically-pure inhibitors (3a–d) strongly suggest that a specific stereo-isomer of the octahydroisochromene scaffold, (1S, 3S) 3b, directs the P1 site imidazole, the warhead aldehyde, and substituent at the 1-position of the fused ring to their appropriate pockets in the protease. To access whether the octahydroisochromene derivatives containing substituents at the 1-position of the ring system function as a novel inhibitor scaffold, the inhibitory activity of compounds 16a-d toward SARS 3CL pro was preliminary evaluated by the IC 50 values obtained using the procedure described below. To determine the configuration of each diastereomer (13a and 13b), the major product obtained after the asymmetric dihydroxylation reaction using (DHQ) 2 Pyr as the chiral ligand (Table 2, entry 3) was isolated and purified using preparative thin layer chromatography (PTLC). ./cache/cord-321858-c5m4dj9m.txt ./txt/cord-321858-c5m4dj9m.txt