The discovery of rofecoxib, [MK 966, VIOXX®, 4-(4′-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2 inhibitor Petpiboon Prasit , Zhaoyin Wang , Christine Brideau , Chi-Chung Chan , Stella Charleson , Wanda Cromlish , Diane Ethier , Jillian F. Evans , Anthony W. Ford-Hutchinson , Jacques-Yves Gauthier , R. Gordon , Jocelyne Guay , Michael J. Gresser , Stacia Kargman , Brian P. Kennedy , Yves Leblanc , Serge Leger , Joseph A. Mancini , Gary P. O'Neill , Marc Ouellet , M.D. Percival , Helene Perrier , Denis Riendeau , Ian W. Rodger , Philip Tagari , Michael J. Therien , Philip J. Vickers , E. Wong , Lijing Xu , Robert N. Young , Robert Zamboni , Susan Boyce , Nadia M.J. Rupniak , Michael J. Forrest , Denise M. Visco , D Patrick Bioorganic & Medicinal Chemistry Letters（1999）
摘要
The development of a COX-2 inhibitor rofecoxib (MK 966, Vioxx) is described. It is essentially equipotent to indomethacin both in vitro and in vivo but without the ulcerogenic side effect due to COX-1 inhibition.
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