Discovery of BI-2545: A Novel Autotaxin Inhibitor That Significantly Reduces LPA Levels in Vivo was written by Kuttruff, Christian A.;Ferrara, Marco;Bretschneider, Tom;Hoerer, Stefan;Handschuh, Sandra;Nosse, Bernd;Romig, Helmut;Nicklin, Paul;Roth, Gerald J.. And the article was included in ACS Medicinal Chemistry Letters in 2017.Formula: C9H10Cl3N This article mentions the following:
In an effort to find new therapeutic interventions addressing the unmet medical need of patients with idiopathic pulmonary fibrosis, we initiated a program to identify new autotaxin (ATX) inhibitors. Starting from a recently published compound (PF-8380), we identified several highly potent ATX inhibitors with improved pharmacokinetic and safety profiles. Further optimization efforts resulted in the identification of a single-digit nanomolar lead compound (BI-2545) that shows substantial lowering of LPA in vivo and is therefore considered a valuable tool for further studies. In the experiment, the researchers used many compounds, for example, 5,7-Dichloro-1,2,3,4-tetrahydroisoquinoline hydrochloride (cas: 73075-47-5Formula: C9H10Cl3N).
5,7-Dichloro-1,2,3,4-tetrahydroisoquinoline hydrochloride (cas: 73075-47-5) belongs to tetrahydroisoquinoline derivatives. The tetrahydroisoquinoline skeleton is present in a number of drugs, such as tubocurarine, one of the quaternary ammonium muscle relaxants. Because of the high biological relevance of compounds possessing the 1,2,3,4-tetrahydroisoquinoline framework, a large number of synthetic approaches towards the creation of an isoquinoline or 1,2,3,4-tetrahydroisoquinoline core are presently known. However, synthetic routes to tetrahydroisoquinoline derivatives containing fluorine atom(s) in their structure are not particularly abundant.Formula: C9H10Cl3N
Referemce:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem