alpha-Alkyl-alpha-amino-beta-sulphone hydroxamates as potent MMP inhibitors that spare MMP-1.

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Becker DP, DeCrescenzo G, Freskos J, Getman DP, Hockerman SL, Li M, Mehta P, Munie GE, Swearingen C

alpha-Alkyl-alpha-amino-beta-sulphone hydroxamates as potent MMP inhibitors that spare MMP-1.

Bioorg Med Chem Lett. 2001 Oct 22;11(20):2723-5.

PubMed ID

11591510 [ View in PubMed

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Abstract

A series of alpha-alkyl-alpha-amino-beta-sulphone hydroxamates was prepared and evaluated for potency versus MMP-2 and MMP-13, and for selectivity versus MMP-1. Low nanomolar potency was obtained with selectivity versus MMP-1 ranging from >10 to >1000. Selected compounds were orally bioavailable.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Marimastat	72 kDa type IV collagenase	IC 50 (nM)	0.75	N/A	N/A	Details
Marimastat	Collagenase 3	IC 50 (nM)	2	N/A	N/A	Details
Marimastat	Interstitial collagenase	IC 50 (nM)	2.9	N/A	N/A	Details