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Design, Synthesis, and Biological Activity Studies of Istradefylline Derivatives Based on Adenine as A 2A Receptor Antagonists.
- Source :
-
ACS omega [ACS Omega] 2021 Feb 04; Vol. 6 (6), pp. 4386-4394. Date of Electronic Publication: 2021 Feb 04 (Print Publication: 2021). - Publication Year :
- 2021
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Abstract
- Due to its double bond, istradefylline rapidly isomerizes to Z -istradefylline when exposed to normal daylight in dilute solution. To solve the poor photostability of the istradefylline solution, a series of istradefylline derivatives (in total 17 compounds, including II-1 and II-2 series) were designed and synthesized, and their biological activity in inhibiting cAMP was evaluated. The IC <subscript>50</subscript> values of compounds II-1-3, II-2-1, II-2-2, II-2-3, II-2-4, and II-2-6 were 7.71, 6.52, 6.16, 7.23, 7.96, and 9.68 μg/mL, respectively, which had the same order of activity as that of istradefylline (IC <subscript>50</subscript> value was 1.94 μg/mL). The preliminary structure-activity relationship suggested that the 6-amino in adenine played an important role in binding an A <subscript>2A</subscript> receptor. The results of photostability experiments showed that the photostability of the target compounds of II-1 and II-2 series was improved when compared with that of istradefylline.<br />Competing Interests: The authors declare no competing financial interest.<br /> (© 2021 The Authors. Published by American Chemical Society.)
Details
- Language :
- English
- ISSN :
- 2470-1343
- Volume :
- 6
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- ACS omega
- Publication Type :
- Academic Journal
- Accession number :
- 33644551
- Full Text :
- https://doi.org/10.1021/acsomega.0c05741