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Design, Synthesis, and Antiviral Activity of the Thiazole Positional Isomers of a Potent HIV-1 Entry Inhibitor NBD-14270статья
- Авторы: Kurkin Alexander V., Curreli Francesca, Iusupov Ildar R., Spiridonov Evgeniy A., Ahmed Shahad, Markov Pavel O., Manasova Ekaterina V., Altieri Andrea, Debnath Asim K.
- Журнал: ChemMedChem
- Год издания: 2022
- Издательство: Wiley - V C H Verlag GmbbH & Co.
- Местоположение издательства: Germany
- DOI: 10.1002/cmdc.202200344
- Аннотация: The envelope glycoprotein gp120 of human immunodeficiency virus type 1 (HIV-1) plays a critical role in virus entry to the cells by binding to the host cellular protein CD4. Earlier, we reported the design and discovery of a series of highly potent small-molecule entry antagonists containing a thiazole ring (Scaffold A). Since this thiazole ring connected with an ethyl amide linkage represents the molecule‘s flexible part, we decided to explore substituting Scaffold A with two other positional isomers of the thiazole ring (Scaffold B and C) to evaluate their effect on the antiviral potency and cellular toxicity. Here we report the novel synthesis of two sets of positional thiazole isomers of the NBD-14270 by retrosynthetic analysis approach, their anti-HIV-1 activity, cellular toxicity, and structure-activity relationships. The study revealed that Scaffold A provided the best HIV-1 inhibitors with higher potency and better selectivity index (SI).
- Добавил в систему: Куркин Александр Витальевич