A simple synthesis of biaryl phospholipase A2 inhibitors: Probing hydrophobic effects

✍ Scribed by Dane M. Springer; Joanne J. Bronson; Muzammil M. Mansuri; David O. Nettleton; Kenneth M. Tramposch

• Book ID: 104364645
• Publisher: Elsevier Science
• Year: 1996
• Tongue: English
• Weight: 217 KB
• Volume: 6
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/s0960-894x(96)00499-4

✦ Synopsis

A series of biaryl acids has been synthesized by treating diphenic anhydride with a variety of amines. The one step strategy allows the rapid interchange of groups for evaluating the hydrophobic constraints of inhibitors of phopholipase A2. The most active inhibitor synthesized displayed an IC50 = 6 IxM against human platelet phospholipase A2.