Synthesis of (+/-) ibuprofen sugar derivatives / 药学学报
Acta Pharmaceutica Sinica
;
(12): 105-109, 2004.
Article
in Chinese
| WPRIM
| ID: wpr-301137
ABSTRACT
<p><b>AIM</b>(+/-) Ibuprofen sugar derivatives were prepared in order to decrease side-effects and increase bioavailability of (+/-) ibuprofen.</p><p><b>METHODS</b>The synthesis of derivatives were performed using 1,23, 4-di-O-isopropylidene-beta-D-galactopyranose, 1,3,4,5-tetra-O-acetyl-2-deoxy-2-amino-beta-D-gluctopyranose, 3,4 6-tri-O-acetyl-2-deoxy-2-N-acetyl-beta-D-gluctosylamine and 2,3,6,2',3',4',6'-hepta-O-acetyl-beta-D-lactosylamine as glycosyl donors, respectively. Target products (4, 7, 12a, 12b, 13) were obtained after deprotection.</p><p><b>RESULTS</b>Five compounds (4, 7, 12a, 12b, 13) were synthesized as new compounds. The structures of all objective compounds were confirmed by 1HNMR, 13CNMR, HMQC, COSY, IR and MS.</p><p><b>CONCLUSION</b>It was found that 12a showed better anti-inflammatory activity than (+/-) ibuprofen.</p>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Molecular Structure
/
Random Allocation
/
Anti-Inflammatory Agents, Non-Steroidal
/
Ibuprofen
/
Therapeutic Uses
/
Drug Therapy
/
Inflammation
/
Molecular Conformation
Limits:
Animals
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2004
Type:
Article
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