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(2R)-N~4~-hydroxy-2-(3-hydroxybenzyl)-N~1~-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide
- Development stage
- Preclinical
- Lead developer
- Pfizer
- Modality
- Small Molecules
01
Overview
(2R)-N~4~-hydroxy-2-(3-hydroxybenzyl)-N~1~-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide is an experimental small molecule inhibitor belonging to the butanediamide and indane compound classes[5][6]. It was developed as a selective inhibitor of aggrecanases ADAMTS‑4 and ADAMTS‑5—metalloproteases implicated in cartilage degradation in osteoarthritis. Structural studies show that its selectivity for aggrecanases over other metalloproteinases is due to subtle factors such as water bridging and protein conformation flexibility rather than direct zinc chelation or charge interactions[8]. The compound has been studied primarily for its potential use in treating osteoarthritis by inhibiting cartilage breakdown[9].
- Other names
- (2R)-N'-hydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-indan-1-yl]-2-(3-hydroxybenzyl)butanediamideN*4*-Hydroxy-2-(3-hydroxy-benzyl)-N*1*-(2-hydroxy-indan-1 yl)-succinamide
02
Targets
ADAMTS5 (A disintegrin and metalloproteinase with thrombospondin motifs 5)ADAMTS4 (ADAM metallopeptidase with thrombospondin type 1 motif 4)
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