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Design and synthesis of potent and selective aldose reductase inhibitors based on pyridylthiadiazine scaffold
- Source :
-
European Journal of Medicinal Chemistry . May2011, Vol. 46 Issue 5, p1536-1544. 9p. - Publication Year :
- 2011
-
Abstract
- Abstract: A series of pyrido[2,3-e]-[1,2,4]-thiadiazine 1,1-dioxide acetic acid derivatives were synthesized and tested for their inhibitory activity against aldose reductase (ALR2). These derivatives were found to be potent aldose reductase inhibitors with IC50 values ranging from 0.038μM to 11.29μM. Most but not all of them showed a strong ALR2 inhibition activity and significant selectivity, which were further supported by docking studies. Of these inhibitors, compound 7d exhibited highest inhibition activity. Structure–activity relationship studies indicate the requirement of N2-benzyl group with electron-withdrawing substituents and N4-acetic acid group in the pyridothiadiazine scaffold. [Copyright &y& Elsevier]
Details
- Language :
- English
- ISSN :
- 02235234
- Volume :
- 46
- Issue :
- 5
- Database :
- Academic Search Index
- Journal :
- European Journal of Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 59639437
- Full Text :
- https://doi.org/10.1016/j.ejmech.2011.01.072