Improvement of the transactivation activity of phenylpropanoic acid-type peroxisome proliferator-activated receptor pan agonists: Effect of introduction of fluorine at the linker part

Jun ichi Kasuga; Takuji Oyama; Yuko Hirakawa; Makoto Makishima; Kosuke Morikawa; Yuichi Hashimoto; Hiroyuki Miyachi

doi:10.1016/j.bmcl.2008.07.046

Improvement of the transactivation activity of phenylpropanoic acid-type peroxisome proliferator-activated receptor pan agonists: Effect of introduction of fluorine at the linker part

Jun ichi Kasuga, Takuji Oyama, Yuko Hirakawa, Makoto Makishima, Kosuke Morikawa, Yuichi Hashimoto, Hiroyuki Miyachi

Faculty of Pharmaceutical Sciences

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

10 Citations (Scopus)

Abstract

We developed a potent peroxisome proliferator-activated receptor pan agonist (a candidate drug for treatment of altered metabolic homeostasis) by introducing fluorine atoms at appropriate position(s) of the known phenylpropionic acid-type pan agonist TIPP-703.

Original language	English
Pages (from-to)	4525-4528
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	16
DOIs	https://doi.org/10.1016/j.bmcl.2008.07.046
Publication status	Published - Aug 15 2008

Keywords

Fluorine
PPAR
PPAR pan agonist

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Access to Document

10.1016/j.bmcl.2008.07.046

Cite this

Kasuga, J. I., Oyama, T., Hirakawa, Y., Makishima, M., Morikawa, K., Hashimoto, Y., & Miyachi, H. (2008). Improvement of the transactivation activity of phenylpropanoic acid-type peroxisome proliferator-activated receptor pan agonists: Effect of introduction of fluorine at the linker part. Bioorganic and Medicinal Chemistry Letters, 18(16), 4525-4528. https://doi.org/10.1016/j.bmcl.2008.07.046

Improvement of the transactivation activity of phenylpropanoic acid-type peroxisome proliferator-activated receptor pan agonists: Effect of introduction of fluorine at the linker part. / Kasuga, Jun ichi; Oyama, Takuji; Hirakawa, Yuko et al.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 18, No. 16, 15.08.2008, p. 4525-4528.

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

Kasuga, JI, Oyama, T, Hirakawa, Y, Makishima, M, Morikawa, K, Hashimoto, Y & Miyachi, H 2008, 'Improvement of the transactivation activity of phenylpropanoic acid-type peroxisome proliferator-activated receptor pan agonists: Effect of introduction of fluorine at the linker part', Bioorganic and Medicinal Chemistry Letters, vol. 18, no. 16, pp. 4525-4528. https://doi.org/10.1016/j.bmcl.2008.07.046

@article{fcff4f39cd8d4dbb99fe25252687271c,

title = "Improvement of the transactivation activity of phenylpropanoic acid-type peroxisome proliferator-activated receptor pan agonists: Effect of introduction of fluorine at the linker part",

abstract = "We developed a potent peroxisome proliferator-activated receptor pan agonist (a candidate drug for treatment of altered metabolic homeostasis) by introducing fluorine atoms at appropriate position(s) of the known phenylpropionic acid-type pan agonist TIPP-703.",

keywords = "Fluorine, PPAR, PPAR pan agonist",

author = "Kasuga, {Jun ichi} and Takuji Oyama and Yuko Hirakawa and Makoto Makishima and Kosuke Morikawa and Yuichi Hashimoto and Hiroyuki Miyachi",

note = "Funding Information: The work described in this letter was partially supported by a Grant-in-aid for Scientific Research from the Ministry of Education, Culture, Sports, Science and Technology, Japan, and grant from Keimeikai Foundation.",

year = "2008",

month = aug,

day = "15",

doi = "10.1016/j.bmcl.2008.07.046",

language = "English",

volume = "18",

pages = "4525--4528",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Limited",

number = "16",

}

TY - JOUR

T1 - Improvement of the transactivation activity of phenylpropanoic acid-type peroxisome proliferator-activated receptor pan agonists

T2 - Effect of introduction of fluorine at the linker part

AU - Kasuga, Jun ichi

AU - Oyama, Takuji

AU - Hirakawa, Yuko

AU - Makishima, Makoto

AU - Morikawa, Kosuke

AU - Hashimoto, Yuichi

AU - Miyachi, Hiroyuki

N1 - Funding Information: The work described in this letter was partially supported by a Grant-in-aid for Scientific Research from the Ministry of Education, Culture, Sports, Science and Technology, Japan, and grant from Keimeikai Foundation.

PY - 2008/8/15

Y1 - 2008/8/15

N2 - We developed a potent peroxisome proliferator-activated receptor pan agonist (a candidate drug for treatment of altered metabolic homeostasis) by introducing fluorine atoms at appropriate position(s) of the known phenylpropionic acid-type pan agonist TIPP-703.

AB - We developed a potent peroxisome proliferator-activated receptor pan agonist (a candidate drug for treatment of altered metabolic homeostasis) by introducing fluorine atoms at appropriate position(s) of the known phenylpropionic acid-type pan agonist TIPP-703.

KW - Fluorine

KW - PPAR

KW - PPAR pan agonist

UR - http://www.scopus.com/inward/record.url?scp=48649098099&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=48649098099&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2008.07.046

DO - 10.1016/j.bmcl.2008.07.046

M3 - Article

C2 - 18662876

AN - SCOPUS:48649098099

SN - 0960-894X

VL - 18

SP - 4525

EP - 4528

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 16

ER -

Improvement of the transactivation activity of phenylpropanoic acid-type peroxisome proliferator-activated receptor pan agonists: Effect of introduction of fluorine at the linker part

Abstract

Keywords

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this