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

Hyup, Yung Hyup; Kwan, Jin Kwan; Kang, Seon-Hwa; Noh, Min-Soo; Ha, Jun-Yong; Kyu, Jin Kyu; Min, Kyung Min; Hoon, Chang Hoon; Chung, Shin.

Bioorg Med Chem Lett ; 13(3): 413-7, 2003 Feb 10.

Article in English | MEDLINE | ID: mdl-12565941

ABSTRACT

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.

Subject(s)

Benzopyrans/chemical synthesis , Benzopyrans/pharmacology , Cyclooxygenase Inhibitors/chemical synthesis , Cyclooxygenase Inhibitors/pharmacology , Isoenzymes/metabolism , Prostaglandin-Endoperoxide Synthases/metabolism , Animals , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Carrageenan , Chemical Phenomena , Chemistry, Physical , Cyclooxygenase 1 , Cyclooxygenase 2 , Cyclooxygenase 2 Inhibitors , Cyclooxygenase Inhibitors/pharmacokinetics , Edema/chemically induced , Edema/prevention & control , Indicators and Reagents , Male , Membrane Proteins , Rats , Rats, Sprague-Dawley

ABSTRACT

Subject(s)

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