Bioorganic & Medicinal Chemistry Letters
A series of α-amino-β-sulphone hydroxamates was prepared and evaluated for potency versus MMP-13 and selectivity versus MMP-1. Various substituents were employed on the α-amino group (P1 position), as well as different groups attached to the sulphone group extending into P1′. Low nanomolar potency was obtained for MMP-13 with selectivity versus MMP-1 of >1000× for a number of analogues.
α-Amino-β-sulphone hydroxamates were prepared, which are potent MMP-13 inhibitors with selectivity versus MMP-1 of >1000× for a number of analogues. Selected compounds exhibited oral bioavailability.
Becker, Daniel P. Ph.D.; Barta, Thomas E.; Bedell, Louis; DeCrescenzo, Gary; Freskos, John; Getman, Daniel P.; Hockerman, Susan L.; Li, Madeleine; Mehta, Pramod; Mischke, Brent; Munie, Grace E.; Swearingen, Craig; and Villamil, Clara I.. α-Amino-β-sulphone hydroxamates as potent MMP-13 inhibitors that spare MMP-1. Bioorganic & Medicinal Chemistry Letters, 11, 20: 2719-2722, 2001. Retrieved from Loyola eCommons, Chemistry: Faculty Publications and Other Works, http://dx.doi.org/10.1016/S0960-894X(01)00556-X
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© Elsevier, 2001.