Orally Bioavailable Dual MMP-1/MMP-14 Sparing, MMP-13 Selective Alpha-sulfone Hydroxamates

Daniel Becker; Stephen A. Kolodziej; Susan L. Hockerman; Terri L. Boehm; Jeffery N. Carroll

doi:10.1016/j.bmcl.2010.04.130

Orally Bioavailable Dual MMP-1/MMP-14 Sparing, MMP-13 Selective Alpha-sulfone Hydroxamates

Daniel Becker, Stephen A. Kolodziej, Susan L. Hockerman, Terri L. Boehm, Jeffery N. Carroll

Department of Chemistry and Biochemistry

Pfizer Research & Development

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

Abstract

A series of phenyl piperidine α-sulfone hydroxamate derivatives has been prepared utilizing a combination of solution-phase and resin-bound library technologies to afford compounds that are potent and highly selective for MMP-13, are dual-sparing of MMP-1 and MMP-14 (MT1-MMP) and exhibit oral bioavailability in rats.

Original language	American English
Journal	Chemistry: Faculty Publications and Other Works
Volume	20
Issue number	12
DOIs	https://doi.org/10.1016/j.bmcl.2010.04.130
State	Published - Jun 15 2010

Keywords

MMP-1
MMP-14
MMP-13
hydroxamates

Disciplines

Chemistry

Access to Document

10.1016/j.bmcl.2010.04.130License: Unspecified

Orally Bioavailable Dual MMP-1 MMP-14 Sparing MMP-13 Selective AFinal published version, 170 KBLicense: Unspecified

Cite this

@article{af6cb6300e5c4d70801d10611a4b4b92,

title = "Orally Bioavailable Dual MMP-1/MMP-14 Sparing, MMP-13 Selective Alpha-sulfone Hydroxamates",

abstract = " A series of phenyl piperidine α-sulfone hydroxamate derivatives has been prepared utilizing a combination of solution-phase and resin-bound library technologies to afford compounds that are potent and highly selective for MMP-13, are dual-sparing of MMP-1 and MMP-14 (MT1-MMP) and exhibit oral bioavailability in rats.",

keywords = "MMP-1, MMP-14, MMP-13, hydroxamates",

author = "Daniel Becker and Kolodziej, \{Stephen A.\} and Hockerman, \{Susan L.\} and Boehm, \{Terri L.\} and Carroll, \{Jeffery N.\}",

year = "2010",

month = jun,

day = "15",

doi = "10.1016/j.bmcl.2010.04.130",

language = "American English",

volume = "20",

journal = "Chemistry: Faculty Publications and Other Works",

number = "12",

}

TY - JOUR

T1 - Orally Bioavailable Dual MMP-1/MMP-14 Sparing, MMP-13 Selective Alpha-sulfone Hydroxamates

AU - Becker, Daniel

AU - Kolodziej, Stephen A.

AU - Hockerman, Susan L.

AU - Boehm, Terri L.

AU - Carroll, Jeffery N.

PY - 2010/6/15

Y1 - 2010/6/15

N2 - A series of phenyl piperidine α-sulfone hydroxamate derivatives has been prepared utilizing a combination of solution-phase and resin-bound library technologies to afford compounds that are potent and highly selective for MMP-13, are dual-sparing of MMP-1 and MMP-14 (MT1-MMP) and exhibit oral bioavailability in rats.

AB - A series of phenyl piperidine α-sulfone hydroxamate derivatives has been prepared utilizing a combination of solution-phase and resin-bound library technologies to afford compounds that are potent and highly selective for MMP-13, are dual-sparing of MMP-1 and MMP-14 (MT1-MMP) and exhibit oral bioavailability in rats.

KW - MMP-1

KW - MMP-14

KW - MMP-13

KW - hydroxamates

UR - https://ecommons.luc.edu/chemistry_facpubs/32

U2 - 10.1016/j.bmcl.2010.04.130

DO - 10.1016/j.bmcl.2010.04.130

M3 - Article

VL - 20

JO - Chemistry: Faculty Publications and Other Works

JF - Chemistry: Faculty Publications and Other Works

IS - 12

ER -

Orally Bioavailable Dual MMP-1/MMP-14 Sparing, MMP-13 Selective Alpha-sulfone Hydroxamates

Abstract

Keywords

Disciplines

Access to Document

Other files and links

Cite this