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New cyclooxygenase-2/5-lipoxygenase inhibitors. 1. 7-tert-buty1-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: discovery and variation of the 5-keto substituent. 1998
J M Janusz, and
P A Young, and
J M Ridgeway, and
M W Scherz, and
K Enzweiler, and
L I Wu, and
L Gan, and
R Darolia, and
R S Matthews, and
D Hennes, and
D E Kellstein, and
S A Green, and
J L Tulich, and
T Rosario-Jansen, and
I J Magrisso, and
K R Wehmeyer, and
D L Kuhlenbeck, and
T H Eichhold, and
R L Dobson, and
S P Sirko, and
R W Farmer
Procter & Gamble Pharmaceuticals, Health Care Research Center, Mason, Ohio 45040, USA.
A series of 5-keto-substituted 7-tert-buty1-2,3-dihydro-3,3- dimethylbenzofurans (DHDMBFs) were prepared and evaluated as potential nonsteroidal antiinflammatory and analgesic agents. Interest in this class of compounds arose when a DHDMBF was found to be an active metabolite of the di-tert-butylphenol antiinflammatory agent tebufelone. We have now found that a variety of 5-keto-substituted DHDMBFs have good in vivo antiinflammatory and analgesic activity after oral administration. These compounds inhibit both cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) in vitro. The cyclooxygenase inhibition was found to be selective for the cyclooxygenase-2 isoform, and this combination of COX-2/5-LOX inhibition may be responsible for the gastrointestinal safety of compounds such as 30.
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P A Young, and
J M Ridgeway, and
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K Enzweiler, and
L I Wu, and
L Gan, and
R Darolia, and
R S Matthews, and
D Hennes, and
D E Kellstein, and
S A Green, and
J L Tulich, and
T Rosario-Jansen, and
I J Magrisso, and
K R Wehmeyer, and
D L Kuhlenbeck, and
T H Eichhold, and
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R W Farmer
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D Hennes, and
D E Kellstein, and
S A Green, and
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R S Matthews, and
D Hennes, and
D E Kellstein, and
S A Green, and
J L Tulich, and
T Rosario-Jansen, and
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P A Young, and
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R S Matthews, and
D Hennes, and
D E Kellstein, and
S A Green, and
J L Tulich, and
T Rosario-Jansen, and
I J Magrisso, and
K R Wehmeyer, and
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Acta crystallographica. Section E, Structure reports online,
