Histidine analogues as potential novel antirheumatic agents.
The relative avidity of novel analogues of histidine for copper chelation, and the ability of such chelates to catalyse the dismutation of the superoxide radical have been assessed using a new in vitro test. The test, designed to detect potential novel antirheumatic agents, was based on a putative mode of action for D-penicillamine. Within the series of histidine analogues, relationships between structure and activity were determined, isohistidine (alpha-amino-2-imidazolepropionic acid) and some of its simple derivatives being particularly active.
Roberts
N A
NA
Roche Products Limited, Welwyn Garden City, Hertfordshire, UK.
Tong
B P
BP
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology; D001172:Arthritis, Rheumatoid / Q000188:drug therapy*; D002614:Chelating Agents; D003300:Copper / Q000032:analysis; D004492:Edetic Acid / Q000494:pharmacology; D006639:Histidine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D006801:Humans; D010396:Penicillamine / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013482:Superoxide Dismutase / Q000037:antagonists & inhibitors
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002614:Chelating Agents; D006639:Histidine; D003300:Copper; D004492:Edetic Acid; D013482:Superoxide Dismutase; D010396:Penicillamine