Kumar, Sanjeev; Waldo, Jesse P.; Jaipuri, Firoz A.; Marcinowicz, Agnieszka; Van Allen, Clarissa; Adams, James; Kesharwani, Tanay; Zhang, Xiaoxia; Metz, Richard; Oh, Angela J.; Harris, Seth F.; Mautino, Mario R. published an article in Journal of Medicinal Chemistry. The title of the article was 《Discovery of Clinical Candidate (1R,4r)-4-((R)-2-((S)-6-Fluoro-5H-imidazo[5,1-a]isoindol-5-yl)-1-hydroxyethyl)cyclohexan-1-ol (Navoximod), a Potent and Selective Inhibitor of Indoleamine 2,3-Dioxygenase 1》.Recommanded Product: Methyl 1-methyl-1H-pyrazole-4-carboxylate The author mentioned the following in the article:
A novel class of 5-substituted 5H-imidazo[5,1-a]isoindoles are described as potent inhibitors of indoleamine 2,3-dioxygenase 1 (IDO1). A structure-based drug design approach was used to elaborate the 5H-imidazo[5,1-a]isoindole core and to improve potency and pharmacol. properties. Suitably placed hydrophobic and polar functional groups in the lead mol. allowed improvement of IDO1 inhibitory activity while minimizing off-target liabilities. Structure-activity relationship studies focused on optimizing IDO1 inhibition potency and a pharmacokinetic profile amenable to oral dosing while controlling CYP450 and hERG inhibitory properties. In the experiment, the researchers used many compounds, for example, Methyl 1-methyl-1H-pyrazole-4-carboxylate(cas: 5952-93-2Recommanded Product: Methyl 1-methyl-1H-pyrazole-4-carboxylate)
Methyl 1-methyl-1H-pyrazole-4-carboxylate(cas: 5952-93-2) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Recommanded Product: Methyl 1-methyl-1H-pyrazole-4-carboxylate
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics