Anti-inflammatory/antiarthritic ketonic bisphosphonic acid esters.
Bisphosphonate ester 2 is an inhibitor of inflammation, but is devoid of antiarthritic effects. SAR studies on a series of related bisphosphonate esters resulted in compounds 6e, 6i, 6j, and 6m, which exhibited excellent inhibition of an arthritis model, in addition to potent anti-inflammatory effects.
Schlachter
S T
ST
Pharmacia & Upjohn, Kalamazoo, MI 49001, USA.
Galinet
L A
LA
Shields
S K
SK
Aspar
D G
DG
Dunn
C J
CJ
Staite
N D
ND
Nugent
R A
RA
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D001169:Arthritis, Experimental / Q000188:drug therapy*; D004164:Diphosphonates / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D015195:Drug Design; D006099:Granuloma / Q000188:drug therapy / Q000276:immunology; D006968:Hypersensitivity, Delayed; D007202:Indicators and Reagents; D007249:Inflammation / Q000188:drug therapy*; D051379:Mice; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004164:Diphosphonates; D007202:Indicators and Reagents