Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors was written by Wurtz, Nicholas R.;Parkhurst, Brandon L.;Jiang, Wen;DeLucca, Indawati;Zhang, Xiaojun;Ladziata, Vladimir;Cheney, Daniel L.;Bozarth, Jeffrey R.;Rendina, Alan R.;Wei, Anzhi;Luettgen, Joseph M.;Wu, Yiming;Wong, Pancras C.;Seiffert, Dietmar A.;Wexler, Ruth R.;Priestley, E. Scott. And the article was included in ACS Medicinal Chemistry Letters in 2016.Application In Synthesis of 7-Nitro-3,4-dihydroisoquinolin-1(2H)-one This article mentions the following:
Inhibitors of Factor VIIa (FVIIa), a serine protease in the clotting cascade, have shown strong antithrombotic efficacy in preclin. thrombosis models with minimal bleeding liabilities. Discovery of potent, orally active FVIIa inhibitors has been largely unsuccessful because known chemotypes have required a highly basic group in the S1 binding pocket for high affinity. A recently reported fragment screening effort resulted in the discovery of a neutral heterocycle, 7-chloro-3,4-dihydroisoquinolin-1(2H)-one, that binds in the S1 pocket of FVIIa and can be incorporated into a phenylglycine FVIIa inhibitor. Optimization of this P1 binding group led to the first series of neutral, permeable FVIIa inhibitors with low nanomolar potency. In the experiment, the researchers used many compounds, for example, 7-Nitro-3,4-dihydroisoquinolin-1(2H)-one (cas: 22245-96-1Application In Synthesis of 7-Nitro-3,4-dihydroisoquinolin-1(2H)-one).
7-Nitro-3,4-dihydroisoquinolin-1(2H)-one (cas: 22245-96-1) belongs to isoquinoline derivatives. Quinoline and its derivatives are widely used as fungicides, biological agents, antibiotics, alkaloids, dyes, rubber chemicals and flavoring agents. Isoquinoline-type alkaloids show biological activities similar to those of morphinane-, protoberberine-, and benzophenanthridine-type alkaloids.Application In Synthesis of 7-Nitro-3,4-dihydroisoquinolin-1(2H)-one
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem