Novel agents combining platelet activating factor (PAF) receptor antagonist with thromboxane synthase inhibitor (TxSI) |
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| Authors: | Fujita Masakazu Seki Taketsugu Inada Haruaki Shimizu Kazuhiro Takahama Akane Sano Tetsuro |
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| Institution: | Omiya Research Laboratory, Nikken Chemicals Co., Ltd., 1-346, Kitabukuro-cho, Saitama-shi, 330-0835, Saitama, Japan. souyaku@jade.dti.ne.jp |
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| Abstract: | Compounds 1 or 2 which possess dual-acting PAF antagonist/TxSI in a previous paper were modified and evaluated for the dual-acting activity. It was found that several compounds were potent dual-acting PAF antagonist/TxSI in and ex vivo. 6-(2-Chlorophenyl)-3-4-(E/Z)-6-ethoxycarbonyl-1-(3-pyridyl)-1-hexenyl]phenylmethyl]-8,11-dimethyl-2,3,4,5-tetrahydro-8H-pyrido4',3': 4,5]thieno3,2-f]triazolo4,3-a]diazepine (12) is excellent orally dual-acting PAF antagonist/TxSI. |
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