Synthesis and evaluation of new 2,6-diamino-5-hetarylpyrimidines as inhibitors of dihydrofolate reductase
Synthetic approaches for the preparation of 6-amino-5-hetarylpyrimidine derivatives by the ring transformation reaction of 2-hetaryl-2-(tetrahydro-2-furanyliden)acetonitriles with amidines have been developed. Some of 2,6-diamino-5-(1,3-benzothiazol-2-yl)pyrimidines were found to exhibit modest inhi...
Saved in:
Published in | Monatshefte für Chemie Vol. 149; no. 4; pp. 813 - 822 |
---|---|
Main Authors | , , , , , |
Format | Journal Article |
Language | English |
Published |
Vienna
Springer Vienna
01.04.2018
Springer Nature Springer Nature B.V |
Subjects | |
Online Access | Get full text |
Cover
Loading…
Summary: | Synthetic approaches for the preparation of 6-amino-5-hetarylpyrimidine derivatives by the ring transformation reaction of 2-hetaryl-2-(tetrahydro-2-furanyliden)acetonitriles with amidines have been developed. Some of 2,6-diamino-5-(1,3-benzothiazol-2-yl)pyrimidines were found to exhibit modest inhibitory activity against human dihydrofolate reductase. Molecular docking was performed to evaluate the binding mode of compounds of this series in the enzyme’s active site.
Graphical abstract |
---|---|
ISSN: | 0026-9247 1434-4475 |
DOI: | 10.1007/s00706-017-2032-7 |