Structure-activity study on a series of α-glutamic acid scaffold based compounds as new ADAMTS inhibitors

Lijie Peng; Lei Duan; Xiaofeng Liu; Mengjie Shen; Yingjun Li; Jiajie Yan; Honglin Li; Ke Ding

doi:10.1016/j.bmcl.2011.06.009

Structure-activity study on a series of α-glutamic acid scaffold based compounds as new ADAMTS inhibitors

Lijie Peng
, Lei Duan
, Xiaofeng Liu
, Mengjie Shen
, Yingjun Li
, Jiajie Yan
, Honglin Li
, Ke Ding^*

^*Corresponding author for this work

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

9 Scopus citations

Abstract

A series of α-glutamic acid scaffold based 4-(benzamido)-4-(1,3,4- oxadiazol-2-yl) butanoic acids were designed and synthesized as new ADAMTS inhibitors. The compounds dose-dependently inhibited the enzymatic activities of ADAMTS-4 and ADAMTS-5. One of the most active compound 2h potently inhibited ADAMTS-4 and ADAMTS-5 with IC ₅₀ values of 1.2 and 0.8 μM, respectively. These inhibitors may serve as new lead compounds for further development of therapeutics to treat osteoarthritis.

Original language	English
Pages (from-to)	4457-4461
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	21
Issue number	15
DOIs	https://doi.org/10.1016/j.bmcl.2011.06.009
State	Published - 1 Aug 2011
Externally published	Yes

Keywords

ADAMTS
Aggrecanase
Glutamic acid scaffold
Osteoarthritis

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10.1016/j.bmcl.2011.06.009

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title = "Structure-activity study on a series of α-glutamic acid scaffold based compounds as new ADAMTS inhibitors",

abstract = "A series of α-glutamic acid scaffold based 4-(benzamido)-4-(1,3,4- oxadiazol-2-yl) butanoic acids were designed and synthesized as new ADAMTS inhibitors. The compounds dose-dependently inhibited the enzymatic activities of ADAMTS-4 and ADAMTS-5. One of the most active compound 2h potently inhibited ADAMTS-4 and ADAMTS-5 with IC 50 values of 1.2 and 0.8 μM, respectively. These inhibitors may serve as new lead compounds for further development of therapeutics to treat osteoarthritis.",

keywords = "ADAMTS, Aggrecanase, Glutamic acid scaffold, Osteoarthritis",

author = "Lijie Peng and Lei Duan and Xiaofeng Liu and Mengjie Shen and Yingjun Li and Jiajie Yan and Honglin Li and Ke Ding",

year = "2011",

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doi = "10.1016/j.bmcl.2011.06.009",

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T1 - Structure-activity study on a series of α-glutamic acid scaffold based compounds as new ADAMTS inhibitors

AU - Peng, Lijie

AU - Duan, Lei

AU - Liu, Xiaofeng

AU - Shen, Mengjie

AU - Li, Yingjun

AU - Yan, Jiajie

AU - Li, Honglin

AU - Ding, Ke

PY - 2011/8/1

Y1 - 2011/8/1

N2 - A series of α-glutamic acid scaffold based 4-(benzamido)-4-(1,3,4- oxadiazol-2-yl) butanoic acids were designed and synthesized as new ADAMTS inhibitors. The compounds dose-dependently inhibited the enzymatic activities of ADAMTS-4 and ADAMTS-5. One of the most active compound 2h potently inhibited ADAMTS-4 and ADAMTS-5 with IC 50 values of 1.2 and 0.8 μM, respectively. These inhibitors may serve as new lead compounds for further development of therapeutics to treat osteoarthritis.

AB - A series of α-glutamic acid scaffold based 4-(benzamido)-4-(1,3,4- oxadiazol-2-yl) butanoic acids were designed and synthesized as new ADAMTS inhibitors. The compounds dose-dependently inhibited the enzymatic activities of ADAMTS-4 and ADAMTS-5. One of the most active compound 2h potently inhibited ADAMTS-4 and ADAMTS-5 with IC 50 values of 1.2 and 0.8 μM, respectively. These inhibitors may serve as new lead compounds for further development of therapeutics to treat osteoarthritis.

KW - ADAMTS

KW - Aggrecanase

KW - Glutamic acid scaffold

KW - Osteoarthritis

UR - https://www.scopus.com/pages/publications/79960371941

U2 - 10.1016/j.bmcl.2011.06.009

DO - 10.1016/j.bmcl.2011.06.009

M3 - 文章

C2 - 21733683

AN - SCOPUS:79960371941

SN - 0960-894X

VL - 21

SP - 4457

EP - 4461

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 15

ER -

Structure-activity study on a series of α-glutamic acid scaffold based compounds as new ADAMTS inhibitors

Abstract

Keywords

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