Name: 3-(1H-Benzo[d]imidazol-2-yl)propan-1-olOn October 8, 2015 ,《Discovery and Optimization of a Series of Pyrimidine-Based Phosphodiesterase 10A (PDE10A) Inhibitors through Fragment Screening, Structure-Based Design, and Parallel Synthesis》 was published in Journal of Medicinal Chemistry. The article was written by Shipe, William D.; Sharik, Steven S.; Barrow, James C.; McGaughey, Georgia B.; Theberge, Cory R.; Uslaner, Jason M.; Yan, Youwei; Renger, John J.; Smith, Sean M.; Coleman, Paul J.; Cox, Christopher D.. The article contains the following contents:
Screening of a fragment library for PDE10A inhibitors identified a low mol. weight pyrimidine hit with PDE10A Ki of 8700 nM and LE of 0.59. Initial optimization by catalog followed by iterative parallel synthesis guided by X-ray cocrystal structures resulted in rapid potency improvements with minimal loss of ligand efficiency. Compound 15h, with PDE10A Ki of 8.2 pM, LE of 0.49, and >5000-fold selectivity over other PDEs, fully attenuates MK-801-induced hyperlocomotor activity after i.p. dosing. The experimental process involved the reaction of 3-(1H-Benzo[d]imidazol-2-yl)propan-1-ol(cas: 2403-66-9Name: 3-(1H-Benzo[d]imidazol-2-yl)propan-1-ol)
3-(1H-Benzo[d]imidazol-2-yl)propan-1-ol(cas: 2403-66-9) belongs to imidazoles.Although other azole heterocycles are ubiquitous in a wide range of biologically active natural products, imidazole rings occur predominantly in the natural amino acid histidine. Name: 3-(1H-Benzo[d]imidazol-2-yl)propan-1-ol In addition, imidazole rings are part of unnatural cyclic peptides and are used as ester isosteres in peptidomimetic studies.
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem