Synthesis and analgesic properties of 5-acyl-arylhydrazone 1-H pyrazolo [3,4-b] pyridine derivatives
A series of 5-acyl-arylhydrazone 1-H pyrazolo [3,4-b] pyridine derivatives (1), planned by applying classical ring isosterism, were synthesized in order to evaluate the structure-activity relationship (SAR), especially the participation of the structural acyl-arylhydrazone subunit in the analgesia....
Gespeichert in:
Veröffentlicht in: | Pharmaceutica acta Helvetiae 1994-12, Vol.69 (3), p.163-169 |
---|---|
Hauptverfasser: | , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
Zusammenfassung: | A series of 5-acyl-arylhydrazone 1-H pyrazolo [3,4-b] pyridine derivatives (1), planned by applying classical ring isosterism, were synthesized in order to evaluate the structure-activity relationship (SAR), especially the participation of the structural acyl-arylhydrazone subunit in the analgesia. The synthetic route used produced the derivatives 1 in ∼ 40% overall yield, using 9 as key intermediate. The results obtained from this study showed that in general the compounds of this series present a powerful analgesic activity in the test of abdominal contortions induced by acetic acid i.p. in albino mice, indicating the participation of the acyl-arylhydrazone moiety, as well the relevance of the substituent of the aryl ring, in the activity. |
---|---|
ISSN: | 0031-6865 |
DOI: | 10.1016/0031-6865(94)90019-1 |