PTP1B inhibition and antihyperglycemic activity in the ob/ob mouse model of novel 11-arylbenzo[b]naphtho[2,3-d]furans and 11-arylbenzo[b]naphtho[2,3- d]thiophenes

Jay Wrobel, Janet Sredy, Christopher Moxham, Arlene Dietrich, Zenan Li, Diane R. Sawicki, Laura Seestaller, Li Wu, Alan Katz, Donald Sullivan, Cesario Tio, Zhong-Yin Zhang

Research output: Contribution to journalArticle

119 Citations (Scopus)

Abstract

We have reported on a series of novel, potent, and selective PTPase inhibitors that function as oral antidiabetic agents. Compounds 6 and 7 are particularly notable in this regard. They were both low nanomolar inhibitors and lowered glucose in the diabetic ob/ob mouse at doses at or below 10 mg/kg/day, po. Compound 7 generally showed selectivities against other PTPases of greater than 25-fold. These compounds and other analogues are currently being further evaluated.

Original languageEnglish (US)
Pages (from-to)3199-3202
Number of pages4
JournalJournal of Medicinal Chemistry
Volume42
Issue number17
DOIs
StatePublished - Aug 26 1999
Externally publishedYes

Fingerprint

Furans
Thiophenes
Protein Tyrosine Phosphatases
Hypoglycemic Agents
Glucose
naphtho(2,3-b)thiophene

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

PTP1B inhibition and antihyperglycemic activity in the ob/ob mouse model of novel 11-arylbenzo[b]naphtho[2,3-d]furans and 11-arylbenzo[b]naphtho[2,3- d]thiophenes. / Wrobel, Jay; Sredy, Janet; Moxham, Christopher; Dietrich, Arlene; Li, Zenan; Sawicki, Diane R.; Seestaller, Laura; Wu, Li; Katz, Alan; Sullivan, Donald; Tio, Cesario; Zhang, Zhong-Yin.

In: Journal of Medicinal Chemistry, Vol. 42, No. 17, 26.08.1999, p. 3199-3202.

Research output: Contribution to journalArticle

Wrobel, J, Sredy, J, Moxham, C, Dietrich, A, Li, Z, Sawicki, DR, Seestaller, L, Wu, L, Katz, A, Sullivan, D, Tio, C & Zhang, Z-Y 1999, 'PTP1B inhibition and antihyperglycemic activity in the ob/ob mouse model of novel 11-arylbenzo[b]naphtho[2,3-d]furans and 11-arylbenzo[b]naphtho[2,3- d]thiophenes', Journal of Medicinal Chemistry, vol. 42, no. 17, pp. 3199-3202. https://doi.org/10.1021/jm990260v
Wrobel, Jay ; Sredy, Janet ; Moxham, Christopher ; Dietrich, Arlene ; Li, Zenan ; Sawicki, Diane R. ; Seestaller, Laura ; Wu, Li ; Katz, Alan ; Sullivan, Donald ; Tio, Cesario ; Zhang, Zhong-Yin. / PTP1B inhibition and antihyperglycemic activity in the ob/ob mouse model of novel 11-arylbenzo[b]naphtho[2,3-d]furans and 11-arylbenzo[b]naphtho[2,3- d]thiophenes. In: Journal of Medicinal Chemistry. 1999 ; Vol. 42, No. 17. pp. 3199-3202.
@article{86773ed7b066442fb77a3f045173020a,
title = "PTP1B inhibition and antihyperglycemic activity in the ob/ob mouse model of novel 11-arylbenzo[b]naphtho[2,3-d]furans and 11-arylbenzo[b]naphtho[2,3- d]thiophenes",
abstract = "We have reported on a series of novel, potent, and selective PTPase inhibitors that function as oral antidiabetic agents. Compounds 6 and 7 are particularly notable in this regard. They were both low nanomolar inhibitors and lowered glucose in the diabetic ob/ob mouse at doses at or below 10 mg/kg/day, po. Compound 7 generally showed selectivities against other PTPases of greater than 25-fold. These compounds and other analogues are currently being further evaluated.",
author = "Jay Wrobel and Janet Sredy and Christopher Moxham and Arlene Dietrich and Zenan Li and Sawicki, {Diane R.} and Laura Seestaller and Li Wu and Alan Katz and Donald Sullivan and Cesario Tio and Zhong-Yin Zhang",
year = "1999",
month = "8",
day = "26",
doi = "10.1021/jm990260v",
language = "English (US)",
volume = "42",
pages = "3199--3202",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "17",

}

TY - JOUR

T1 - PTP1B inhibition and antihyperglycemic activity in the ob/ob mouse model of novel 11-arylbenzo[b]naphtho[2,3-d]furans and 11-arylbenzo[b]naphtho[2,3- d]thiophenes

AU - Wrobel, Jay

AU - Sredy, Janet

AU - Moxham, Christopher

AU - Dietrich, Arlene

AU - Li, Zenan

AU - Sawicki, Diane R.

AU - Seestaller, Laura

AU - Wu, Li

AU - Katz, Alan

AU - Sullivan, Donald

AU - Tio, Cesario

AU - Zhang, Zhong-Yin

PY - 1999/8/26

Y1 - 1999/8/26

N2 - We have reported on a series of novel, potent, and selective PTPase inhibitors that function as oral antidiabetic agents. Compounds 6 and 7 are particularly notable in this regard. They were both low nanomolar inhibitors and lowered glucose in the diabetic ob/ob mouse at doses at or below 10 mg/kg/day, po. Compound 7 generally showed selectivities against other PTPases of greater than 25-fold. These compounds and other analogues are currently being further evaluated.

AB - We have reported on a series of novel, potent, and selective PTPase inhibitors that function as oral antidiabetic agents. Compounds 6 and 7 are particularly notable in this regard. They were both low nanomolar inhibitors and lowered glucose in the diabetic ob/ob mouse at doses at or below 10 mg/kg/day, po. Compound 7 generally showed selectivities against other PTPases of greater than 25-fold. These compounds and other analogues are currently being further evaluated.

UR - http://www.scopus.com/inward/record.url?scp=13044270997&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=13044270997&partnerID=8YFLogxK

U2 - 10.1021/jm990260v

DO - 10.1021/jm990260v

M3 - Article

C2 - 10464006

AN - SCOPUS:13044270997

VL - 42

SP - 3199

EP - 3202

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 17

ER -