Synthesis and anti-inflammatory analgesic activities of phenylfuroxan-coupled diclofenac / 药学学报
Acta Pharmaceutica Sinica
;
(12): 27-32, 2002.
Article
in Chinese
| WPRIM
| ID: wpr-343407
ABSTRACT
<p><b>AIM</b>To search for new derivatives of diclofenac (DC) having higher potency than the parent drug and lacking its undesirable effects.</p><p><b>METHODS</b>Coupling DC with NO donor 3-hydroxymethyl-4-phenylfuroxan and its isomer through esterification, evaluating anti-inflammatory and analgesic activities, observing side effects in the rat gastrointestinal (GI) tract and assessing NO releasing ability both in vitro and in vivo.</p><p><b>RESULTS</b>Fifteen new compounds including nine target ones (II1-9) were synthesized, and their structures were determined by IR, 1HNMR, MS and elemental analysis. Compounds II3 and II9 showed anti-inflammatory activity comparable to DC. Compound II2 showed stronger anti-inflammatory and analgesic activities and less GI side effect than DC, and released NO in vivo.</p><p><b>CONCLUSION</b>Compound II2 is worthy to be intensively studied.</p>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Oxadiazoles
/
Pharmacology
/
Structure-Activity Relationship
/
Molecular Structure
/
Chemistry
/
Anti-Inflammatory Agents, Non-Steroidal
/
Diclofenac
/
Pain Threshold
/
Nitric Oxide Donors
/
Cyclic N-Oxides
Limits:
Animals
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2002
Type:
Article
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