Inhibitors of immune complex-induced inflammation: 5-substituted 3-[1-(2-benzoxazolyl)hydrazino]propanenitrile derivatives.
A number of 5-substituted 3-[1-(2-benzoxazolyl)hydrazino]propanenitrile analogues have been studied as inhibitors of the rat pleural reverse passive Arthus reaction, and quantitative structure-activity relationships (QSAR) of these analogues have been examined. The QSAR equations indicate that hydrophilic substituents at the 5-position produce more potent compounds, while electron-releasing groups decrease activity. The results supplement QSAR data we previously obtained from the dermal reverse passive Arthus reaction.
Kim
K H
KH
Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064.
Martin
Y C
YC
Young
P R
PR
Carter
G W
GW
Haviv
F
F
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000627:therapeutic use*; D001183:Arthus Reaction / Q000276:immunology; D001583:Benzoxazoles / Q000627:therapeutic use*; D005122:Exudates and Transudates / Q000166:cytology; D006834:Hydrazines / Q000627:therapeutic use; D007105:Immune Complex Diseases / Q000150:complications / Q000188:drug therapy*; D007249:Inflammation / Q000188:drug therapy* / Q000209:etiology; D007958:Leukocyte Count; D008297:Male; D009570:Nitriles / Q000627:therapeutic use*; D051381:Rats; D013329:Structure-Activity Relationship
D000894:Anti-Inflammatory Agents, Non-Steroidal; D001583:Benzoxazoles; D006834:Hydrazines; D009570:Nitriles