Simultaneous biological optimization and structural simplification of a pendant heterocyclic thiobenzimidazolone on a series of 2-phenyl-4-(piperazin-1-yl)benzimidazole antagonists of the Gonadotropin Releasing Hormone Receptor

被引：0

作者：

Pelletier, Jeffrey C. ^{[1
]}

Chengalvala, Murty V. ^{[2
]}

Cottom, Joshua E. ^{[2
]}

Garrick, Lloyd ^{[1
]}

Jetter, James ^{[1
]}

Kao, Wenling ^{[1
]}

Shanno, Linda ^{[2
]}

Wrobel, Jay ^{[3
]}

机构：

[1] Wyeth Res, Dept Chem & Screening Sci, Collegeville, PA 19426 USA

[2] Wyeth Res, Dept Womens Hlth & Musculoskeletal Biol, Collegeville, PA 19426 USA

[3] Wyeth Res, Chem & Screening Sci, Collegeville, PA 19426 USA

来源：

ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY | 2007年 / 234卷

关键词：

D O I：

暂无

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

80-MEDI

引用

页数：1

共 4 条

[1] Structure activity relationships of the linker group in 2-phenyl-4-piperazinyl-benzimidazole antagonists of the Gonadotropin-Releasing Hormone Receptor (GnRH)
Hauze, Diane B.
Pelletier, Jeffrey C.
Mann, Charles W.
Green, Daniel
Rogers, John
Chengalvala, Murty V.
Cottom, Joshua E.
Shanno, Linda
Feingold, Irene B.
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2006, 231
[2] Small molecule antagonists of the gonadotropin-releasing hormone (GnRH) receptor: Structure-activity relationships of small heterocyclic groups appended to the 2-phenyl-4-piperazinyl-benzimidazole template
Hauze, Diane B.
Chengalvala, Murty V.
Cottom, Joshua E.
Feingold, Irene B.
Garrick, Lloyd
Green, Daniel M.
Huselton, Christine
Kao, Wenling
Kees, Kenneth
Lundquist, Joseph T.
Mann, Charles W.
Mehlmann, John F.
Rogers, John F.
Shanno, Linda
Wrobel, Jay
Pelletier, Jeffrey C.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (07) : 1986 - 1990
[3] Discovery of 6-({4-[2-(4-tert-Butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): An Orally Active Antagonist of the Gonadotropin Releasing Hormone Receptor (GnRH-R)
Pelletier, Jeffrey C.
Chengalvala, Murty V.
Cottom, Joshua E.
Feingold, Irene B.
Green, Daniel M.
Hauze, Diane B.
Huselton, Christine A.
Jetter, James W.
Kopf, Gregory S.
Lundquist, Joseph T., IV
Magolda, Ronald L.
Mann, Charles W.
Mehlmann, John F.
Rogers, John F.
Shanno, Linda K.
Adams, William R.
Tio, Cesario O.
Wrobel, Jay E.
JOURNAL OF MEDICINAL CHEMISTRY, 2009, 52 (07) : 2148 - 2152
[4] Discovery of 1-{4[1-(2,6-Difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea (TAK-385) as a Potent, Orally Active, Non-Peptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor
Miwa, Kazuhiro
Hitaka, Takenori
Imada, Takashi
Sasaki, Satoshi
Yoshimatsu, Mie
Kusaka, Masami
Tanaka, Akira
Nakata, Daisuke
Furuya, Shuichi
Endo, Satoshi
Hamamura, Kazumasa
Kitazaki, Tomoyuki
JOURNAL OF MEDICINAL CHEMISTRY, 2011, 54 (14) : 4998 - 5012

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