The rational design of novel 5-amino-2-oxindole derivatives with antiglaucomic activity

Bioorg Med Chem Lett. 2023 May 17:129334. doi: 10.1016/j.bmcl.2023.129334. Online ahead of print.ABSTRACTCompounds with a 2-oxindole scaffold play an important role in organic synthesis and especially in the synthesis of bioactive organic compounds, therefore, the development of new methods for modifying this scaffold is a very interesting and urgent task. In the framework of this study, we have created a rational approach to the synthesis of 5-amino-substituted derivatives of 2-oxindole. The approach is characterized by good total yield and a small number of steps. One-stage modification of obtained 5-amino-2-oxindoles leads to compounds with promising antiglaucomic activity. The most active compound 7a reduce intraocular pressure by 24% in normotensive rabbits (18% for reference drug timolol).PMID:37207847 | DOI:10.1016/j.bmcl.2023.129334

Source: Bioorganic and Medicinal Chemistry Letters - May 19, 2023 Category: Chemistry Authors: Roman O Eremeev Olga V Beznos Alexander M Efremov Natalia B Chesnokova Natalia A Lozinskaya Source Type: research