The development of highly potent and selective small molecule correctors of Z α1-antitrypsin misfolding was written by Liddle, John;Pearce, Andrew C.;Arico-Muendel, Christopher;Belyanskaya, Svetlana;Brewster, Andrew;Brown, Murray;Chung, Chun-wa;Denis, Alexis;Dodic, Nerina;Dossang, Anthony;Eddershaw, Peter;Klimaszewska, Diana;Haq, Imran;Holmes, Duncan S.;Jagger, Alistair;Jakhria, Toral;Jigorel, Emilie;Lind, Ken;Messer, Jeff;Neu, Margaret;Olszewski, Allison;Ronzoni, Riccardo;Rowedder, James;Rudiger, Martin;Skinner, Steve;Smith, Kathrine J.;Trottet, Lionel;Uings, Iain;Zhu, Zhengrong;Irving, James A.;Lomas, David A.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2021.Synthetic Route of C9H7NO3 This article mentions the following:
α1-Antitrypsin deficiency is characterized by the misfolding and intracellular polymerization of mutant α1-antitrypsin protein within the endoplasmic reticulum (ER) of hepatocytes. Small mols. that bind and stabilize Z α1-antitrypsin were identified via a DNA-encoded library screen. A subsequent structure-based optimization led to a series of highly potent, selective and cellular active α1-antitrypsin correctors, e.g., I. In the experiment, the researchers used many compounds, for example, 2-Oxoindoline-4-carboxylic acid (cas: 90322-37-5Synthetic Route of C9H7NO3).
2-Oxoindoline-4-carboxylic acid (cas: 90322-37-5) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Synthetic Route of C9H7NO3
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles