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

Authors

Daniel Becker, Loyola University ChicagoFollow
Gary A. DeCrescenzo
John Freskos
Daniel P. Getman

Document Type

Article

Publication Date

10-22-2001

Publication Title

Bioorganic & Medicinal Chemistry Letters

Volume

11

Issue

20

Pages

2723-2725

Publisher Name

Elsevier

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.

Comments

Author Posting © Elsevier, 2001. This is the author's version of the work. It is posted here by permission of Elsevier for personal use, not for redistribution. The definitive version was published in Bioorganic & Medicinal Chemistry Letters, Volume 11, Issue 20, October 22, 2001. http://dx.doi.org/10.1016/S0960-894X(01)00557-1

Recommended Citation

Becker, Daniel; DeCrescenzo, Gary A.; Freskos, John; and Getman, Daniel P.. Alpha-Alkyl-alpha-amino-beta-sulphone Hydroxamates as Potent MMP Inhibitors that Spare MMP-1. Bioorganic & Medicinal Chemistry Letters, 11, 20: 2723-2725, 2001. Retrieved from Loyola eCommons, Chemistry: Faculty Publications and Other Works, http://dx.doi.org/10.1016/S0960-894X(01)00557-1

Creative Commons License

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Copyright Statement

© 2001 Elsevier