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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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-02, Vol.13 (3), p.413-417
Hauptverfasser:	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:	Artikel
Sprache:	eng
Schlagworte:	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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Zusammenfassung:	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