Alpha-Alkyl-alpha-amino-beta-sulphone Hydroxamates as Potent MMP Inhibitors that Spare MMP-1

Daniel Becker; Gary A. DeCrescenzo; John Freskos; Daniel P. Getman

doi:10.1016/S0960-894X(01)00557-1

Alpha-Alkyl-alpha-amino-beta-sulphone Hydroxamates as Potent MMP Inhibitors that Spare MMP-1

Daniel Becker, Gary A. DeCrescenzo, John Freskos, Daniel P. Getman

Department of Chemistry and Biochemistry

Research output: Contribution to journal › Article › peer-review

Abstract

A series of α-alkyl-α-amino-β-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.

Original language	American English
Journal	Chemistry: Faculty Publications and Other Works
Volume	11
Issue number	20
DOIs	https://doi.org/10.1016/S0960-894X(01)00557-1
State	Published - Oct 22 2001

Keywords

hydroxamates
MMP inhibitors

Disciplines

Chemistry

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title = "Alpha-Alkyl-alpha-amino-beta-sulphone Hydroxamates as Potent MMP Inhibitors that Spare MMP-1",

abstract = " A series of α-alkyl-α-amino-β-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.",

keywords = "hydroxamates, MMP inhibitors",

author = "Daniel Becker and DeCrescenzo, {Gary A.} and John Freskos and Getman, {Daniel P.}",

year = "2001",

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AU - Becker, Daniel

AU - DeCrescenzo, Gary A.

AU - Freskos, John

AU - Getman, Daniel P.

PY - 2001/10/22

Y1 - 2001/10/22

N2 - A series of α-alkyl-α-amino-β-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.

AB - A series of α-alkyl-α-amino-β-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.

KW - hydroxamates

KW - MMP inhibitors

UR - https://ecommons.luc.edu/chemistry_facpubs/20

U2 - 10.1016/S0960-894X(01)00557-1

DO - 10.1016/S0960-894X(01)00557-1

M3 - Article

VL - 11

JO - Chemistry: Faculty Publications and Other Works

JF - Chemistry: Faculty Publications and Other Works

IS - 20

ER -

Alpha-Alkyl-alpha-amino-beta-sulphone Hydroxamates as Potent MMP Inhibitors that Spare MMP-1

Abstract

Keywords

Disciplines

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