Substituted 4, 6-diaminoquinolines as inhibitors of C5a receptor binding

…, T Rollins, S Siciliano, DN Cianciarulo…

Index: Lanza, Thomas J.; Durette, Philippe L.; Rollins, Thomas; Siciliano, Salvatore; Cianciarulo, Dana N.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 2 p. 252 - 258

Full Text: HTML

Citation Number: 62

Abstract

The anaphylatoxin C5a is implicated in a number of inflammatory diseases. It is a highly cationic protein with 13 of 74 amino acids being either arginine or lysine. A search focusing on pitively charged molecules, particularly amine-containing functionalities, led to the discovery of substituted 4, 6-diaminoquinolines 1 [N, N'-bis (4-amino-2-methyl-6quinolyl) urea] and 7 [6-N-(2-chlorocinnamoyl)-4, 6-diamino-2-methylquinohe) as inhibitors of C5a ...