Carbonyl-containing bisphosphonate esters as novel antiinflammatory and antiarthritic agents

RA Nugent, ST Schlachter, M Murphy…

Index: Nugent; Schlachter; Murphy; Dunn; Staite; Galinet; Shields; Wu; Aspar; Richard Journal of Medicinal Chemistry, 1994 , vol. 37, # 26 p. 4449 - 4454

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Citation Number: 33

Abstract

A study of the decomposition of the pyrazoline bisphosphonate ester 2 identified 3 as the sole bisphosphonate component. Evaluation in a delayed-type hypersensitivity granuloma model of chronic inflammation in mice (DTH-GRA) showed 3 to be a potent inhibitor of granuloma formation (sc, 10 mg/kg, 45%), but in a murine model of antigen-induced arthritis (AIA), no significant inhibition was observed. As a result, new ketonic bisphosphonate ...