Identification of novel urea derivatives as PTP1B inhibitors: synthesis, biological evaluation and structure-activity relationships

被引：10

作者：

Gupta, Swati ^{[1
]}

Varshney, Kanika ^{[1
]}

Srivastava, Rohit ^{[2
]}

Rahuja, Neha ^{[2
]}

Rawat, Arun K. ^{[2
]}

Srivastava, Arvind K. ^{[2
]}

Saxena, Anil K. ^{[1
]}

机构：

[1] Cent Drug Res Inst, CSIR, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India

[2] Cent Drug Res Inst, CSIR, Div Biochem, Lucknow 226001, Uttar Pradesh, India

来源：

MEDCHEMCOMM | 2013年 / 4卷 / 10期

关键词：

TYROSINE-PHOSPHATASE; 1B; INSULIN SENSITIVITY; RESISTANCE; OBESITY; DISCOVERY; DESIGN;

D O I：

10.1039/c3md00138e

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The protein tyrosine phosphatase 1B (PTP1B) is an attractive target for the treatment of type 2 diabetes. A series of substituted 1,3-benzyl urea has been synthesized and evaluated for PTP1B inhibitory, antidiabetic and antidyslipidemic activities. The most active compound of the series 5b showed 79.4% PTP1B inhibition and 20.7% blood glucose lowering in the STZ model. It also lowered the serum cholesterol level by 16.3% and significantly increased the serum HDL-cholesterol by 46.8%. The high activity of compound 5b has been explained by docking studies.

引用

页码：1382 / 1387

页数：6

共 50 条

[1] Discovery and structure-activity relationships of novel sulfonamides as potent PTP1B inhibitors
Holmes, CP
Li, XF
Pan, YJ
Xu, CD
Bhandari, A
Moody, CM
Miguel, JA
Ferla, SW
De Francisco, MN
Frederick, BT
Zhou, SQ
Macher, N
Jang, L
Irvine, JD
Grove, JR
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (19) : 4336 - 4341
[2] Varic acid analogues from fungus as PTP1B inhibitors: Biological evaluation and structure-activity relationships
Sun, Wenlong
Zhuang, Chunlin
Li, Xia
Zhang, Bowei
Lu, Xinhua
Zheng, Zhihui
Dong, Yuesheng
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2017, 27 (15) : 3382 - 3385
[3] Synthesis and Biological Evaluation of Uncharged Chalcone Derivatives as Novel PTP1B Inhibitors
Song, Ming-Xia
Deng, Xian-Qing
LATIN AMERICAN JOURNAL OF PHARMACY, 2018, 37 (01): : 68 - 72
[4] Synthesis and biological evaluation of oleanolic acid derivatives as PTP1B inhibitors
Liu, Qing-Chao
Guo, Tian-Tian
Zhang, Lei
Yu, Yue
Wang, Peng
Yang, Ju-Fang
Li, Ying-Xia
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2013, 63 : 511 - 522
[5] Synthesis and biological evaluation of novel N-(alkoxyphenyl)-aminocarbonylbenzoic acid derivatives as PTP1B inhibitors
Tong, Yuan Feng
Zhang, Pei
Chen, Feng
Hao, Ling Hua
Ye, Fei
Tian, Jin Ying
Wu, Song
CHINESE CHEMICAL LETTERS, 2010, 21 (12) : 1415 - 1418
[6] Synthesis and biological evaluation of novel N-(alkoxyphenyl)-aminocarbonylbenzoic acid derivatives as PTP1B inhibitors
Yuan Feng Tong~a
ChineseChemicalLetters, 2010, 21 (12) : 1415 - 1418
[7] Design, synthesis and biological evaluation of uncharged catechol derivatives as selective inhibitors of PTP1B
Li, Xiang-Qian
Xu, Qi
Luo, Jiao
Wang, Li-Jun
Jiang, Bo
Zhang, Ren-Shuai
Shi, Da-Yong
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2017, 136 : 348 - 359
[8] The first synthesis of natural disulfide bruguiesulfurol and biological evaluation of its derivatives as a novel scaffold for PTP1B inhibitors
Chen, Jing
Jiang, Cheng-Shi
Ma, Wen-Quan
Gao, Li-Xin
Gong, Jing-Xu
Li, Jing-Ya
Li, Jia
Guo, Yue-Wei
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2013, 23 (18) : 5061 - 5065
[9] Synthesis and biological evaluation of novel bis-aromatic amides as novel PTP1B inhibitors
Wang, Wen-Long
Huang, Chao
Gao, Li-Xin
Tang, Chun-Lan
Wang, Jun-Qing
Wu, Min-Chen
Sheng, Li
Chen, Hai-Jun
Nan, Fa-Jun
Li, Jing-Ya
Li, Jia
Feng, Bainian
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2014, 24 (08) : 1889 - 1894
[10] Novel thiophene derivatives as PTP1B inhibitors with selectivity and cellular activity
Ye, Deju
Zhang, Yu
Wang, Fei
Zheng, Mingfang
Zhang, Xu
Luo, Xiaomin
Shen, Xu
Jiang, Hualiang
Liu, Hong
BIOORGANIC & MEDICINAL CHEMISTRY, 2010, 18 (05) : 1773 - 1782

← 1 2 3 4 5 →