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Abstract #109371 Published in IGR 24-1/2
The rational design of novel 5-amino-2-oxindole derivatives with antiglaucomic activity
Eremeev RO; Beznos OV; Efremov AM; Chesnokova NB; Lozinskaya NABioorganic and Medicinal Chemistry Letters 2023; 90: 129334
Compounds 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).
Department of Chemistry, Lomonosov Moscow State University, 119992 Moscow, Russian Federation. Electronic address: roma.chem.dep@mail.ru.
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