2,3-Diarylbenzopyran derivatives as a novel class of selective cyclooxygenase-2 inhibitors

A new series of cyclooxygenase-2(COX-2) inhibitors with naturally occurring flavone as the main skeleton has been synthesized and their biological activities were evaluated for cyclooxygenase inhibitory activity. Rational structural modifications were applied to potent COX-2 inhibitors to obtain the...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-02, Vol.13 (3), p.413-417
Main Authors: Hyup Joo, Yung, Kwan Kim, Jin, Kang, Seon-Hwa, Noh, Min-Soo, Ha, Jun-Yong, Kyu Choi, Jin, Min Lim, Kyung, Hoon Lee, Chang, Chung, Shin
Format: Article
Language:English
Subjects:
Animals
Anti-Inflammatory Agents, Non-Steroidal - pharmacology
Benzopyrans - chemical synthesis
Benzopyrans - pharmacology
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Carrageenan
Chemical Phenomena
Chemistry, Physical
Cyclooxygenase 1
Cyclooxygenase 2
Cyclooxygenase 2 Inhibitors
Cyclooxygenase Inhibitors - chemical synthesis
Cyclooxygenase Inhibitors - pharmacokinetics
Cyclooxygenase Inhibitors - pharmacology
Edema - chemically induced
Edema - prevention & control
Indicators and Reagents
Isoenzymes - metabolism
Male
Medical sciences
Membrane Proteins
Pharmacology. Drug treatments
Prostaglandin-Endoperoxide Synthases - metabolism
Rats
Rats, Sprague-Dawley
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Summary:A new series of cyclooxygenase-2(COX-2) inhibitors with naturally occurring flavone as the main skeleton has been synthesized and their biological activities were evaluated for cyclooxygenase inhibitory activity. Rational structural modifications were applied to potent COX-2 inhibitors to obtain the desired pharmacokinetic profiles for improved oral anti-inflammatory activity. A new series of benzopyrans has been synthesized and tested for cyclooxygenase inhibitory activity. Rational structural modifications were applied to potent COX-2 inhibitors to obtain the desired pharmacokinetic profiles for improved oral anti-inflammatory activity.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(02)00952-6