A practical, Nenitzescu-based synthesis of LY311727, the first potent and selective s-PLA2 inhibitor

…, VV Khau, DR Hutchison, MJ Martinelli

Index: Pawlak; Khau; Hutchison; Martinelli Journal of Organic Chemistry, 1996 , vol. 61, # 25 p. 9055 - 9059

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Citation Number: 36

Abstract

Patients with acute pancreatitis, bacterial peritonitis, adult respiratory distress syndrome (ARDS), septic shock, and arthritis all display extraordinarily high blood levels of secretory phospholipase A2 (s-PLA2). 1 The in vivo trigger for s-PLA2 release under such conditions is mediated by a number of mechanisms, all of which have been investigated as a primary site for drug discovery. However, it is believed that potent and selective inhibitors of s- ...