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KMID : 0617220010120010023
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Duksung Bulletin Phamaceutical Sciences
2001 Volume.12 No. 1 p.23 ~ p.28
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Prostaglandin Synthase-2 Inhibitory Activity of Diazaanthrine Derivatives
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Abstract
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A series of diazaanthrine derivatives (3a-3e) as new analogues of tacrine has been prepared. This series has been tested for their ability to inhibit prostaglandin synthase-1 and 2 isoforms. This series has shown potent in vitro inhibition of the enzyme prostaglandin synthase-2 with ％ inhibition=70.3∼23.6 at 10 ㎍/㎖. Compound 3b was the most potential inhibitor with an IC_50s=15.6 ㎍/㎖. Derivatives 3a and 3c displayed weak in vitro inhibition of prostaglandin synthase-2 with IC_50s 20.2∼29.2 ㎍/㎖. The most selective compound was 3b with a prostaglandin synthase inhibitory activity of 1/2 in excess of 5 times. These data indicate that 3b is an prostaglandin synthase-2 inhibitor with good selectivity as the drug of Alzheimer´s disease.
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