Triazolobenzo-and triazolothienodiazepines as potent antagonists of platelet activating factor

…, C Maresca, B Yaremko, M O'Donnell

Index: Walser; Flynn; Mason; Crowley; Maresca; Yaremko; O'Donnell Journal of Medicinal Chemistry, 1991 , vol. 34, # 3 p. 1209 - 1221

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Citation Number: 37

Abstract

1 2 palladium-catalyzed coupling of acetylenes with aryl iodides or aryl bromides as a possible synthetic route. The pilot reaction, in which N-propargylphthalimide was coupled with 8-iodotriazolobenzodiazepine lob, resulted in compound 17, which surprisingly was found to have excellent activity as a PAF antagonist, surpassing WEB 2086 in our screening tests5 (Table I). Encouraged by these findings we embarked on a search for even more ...

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