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KMID : 0896220010210010269
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Journal of Daegu Health College
2001 Volume.21 No. 1 p.269 ~ p.277
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Structure-Activity Relationship Of 4,5-Diarylpyrroles
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Do Seong-Tak
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Abstract
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The antiinflammatory activity of a series of 2-substituted- and 2,3-disubstituted -4-(4-flurorophenyl)-5-[4-(methylsulfonyl)phenyl]-1H-pyrroles was shown by structure-activity relationship studies to be correlated with the molar refractivity of the 1-substituent and size effect and electronic effect of the 2-substituent. Other molecular descriptors such as ovality, molecular weight and charge contributed to antiinflammatory activity. Much of the anti-inflammatory activity of these pyrroles could be correlated with the inhibition of the isoform of cyclooxygenase(COX2). Additional structure-activity relationship studies have been used to identify the molecular parameters necessary for maximizing COX2 inhibition while simultaneously minimizing the inhibition of constitutively expressed cyclooxygenase-1. Such an effort should facilitate the discovery and development of selective COX inhibitors that should lead to safer nonsteroidal antiinflammatory drugs.
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KEYWORD
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