Discovery of novel N-acylsulfonamide analogs as potent and selective EP3 receptor antagonists

被引：23

作者：

Asada, Masaki ^{[1
]}

Obitsu, Tetsuo ^{[1
]}

Kinoshita, Atsushi ^{[1
]}

Nakai, Yoshihiko ^{[1
]}

Nagase, Toshihiko ^{[1
]}

Sugimoto, Isamu ^{[1
]}

Tanaka, Motoyuki ^{[1
]}

Takizawa, Hiroya ^{[1
]}

Yoshikawa, Ken ^{[1
]}

Sato, Kazutoyo ^{[1
]}

Narita, Masami ^{[1
]}

Ohuchida, Shuichi ^{[1
]}

Nakai, Hisao ^{[1
]}

Toda, Masaaki ^{[1
]}

机构：

[1] Ono Pharmaceut Co Ltd, Minase Res Inst, Osaka 6188585, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 08期

关键词：

Prostaglandin; EP3; receptor; Antagonist; N-Acylsulfonamide; N-Acyl (3,4-difluorobenzene)sulfonamide; PROSTANOID RECEPTOR; MICE LACKING; SUBTYPE; MYOMETRIUM;

D O I：

10.1016/j.bmcl.2010.02.034

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel N-acylsulfonamide analogs were synthesized and evaluated for their binding affinity and antagonist activity for the EP3 receptor subtype. Representative compounds were also evaluated for their inhibitory effect on PGE(2)-induced uterine contraction in pregnant rats. Among those tested, a series of N-acylbenzenesulfonamide analogs were found to be more potent than the corresponding carboxylic acid analogs in both the in vitro and in vivo evaluations. The structure activity relationships (SAR) are also discussed. (C) 2010 Published by Elsevier Ltd.

引用

页码：2639 / 2643

页数：5

共 50 条

[41] Pyrrolidin-3-yl-N-methylbenzamides as potent histamine 3 receptor antagonists
Zhou, Dahui
Gross, Jonathan L.
Sze, Jean Y.
Adedoyin, Adedayo B.
Bowlby, Mark
Di, Li
Platt, Brian J.
Zhang, Guoming
Brandon, Nicholas
Comery, Thomas A.
Robichaud, Albert J.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (19) : 5957 - 5960
[42] Novel Potent Selective Orally Active S1P5 Receptor Antagonists
Ma, Bin
Guckian, Kevin M.
Liu, Xiao-gao
Yang, Chunhua
Li, Bing
Scannevin, Robert
Mingueneau, Michael
Drouillard, Annabelle
Walzer, Thierry
ACS MEDICINAL CHEMISTRY LETTERS, 2021, 12 (03): : 351 - 355
[43] Novel Tetrahydroquinazolinamines as Selective Histamine 3 Receptor Antagonists for the Treatment of Obesity
Kumar, Ajeet
Pasam, Venkata Reddy
Thakur, Ravi Kumar
Singh, Maninder
Singh, Kartikey
Shukla, Mahendra
Yadav, Anubhav
Dogra, Shalini
Sona, Chandan
Umrao, Deepmala
Jaiswal, Swati
Ahmad, Hafsa
Rashid, Mamunur
Singh, Sandeep K.
Wahajuddin, Muhammad
Dwivedi, Anil Kumar
Siddiq, Mohammad Imran
Lal, Jawahar
Tripathi, Rama Pati
Yadav, Prem N.
JOURNAL OF MEDICINAL CHEMISTRY, 2019, 62 (09) : 4638 - 4655
[44] Discovery of novel, non-acidic 1,5-biaryl pyrrole EP1 receptor antagonists
Hall, Adrian
Atkinson, Stephen
Brown, Susan H.
Chessell, Iain P.
Chowdhury, Anita
Giblin, Gerard M. P.
Goldsmith, Paul
Healy, Mark P.
Jandu, Karamjit S.
Johnson, Matthew R.
Michel, Anton D.
Naylor, Alan
Sweeting, Jennifer A.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (05) : 1200 - 1205
[45] Pharmacological properties of ASP7657, a novel, potent, and selective prostaglandin EP4 receptor antagonist
Mizukami, Kazuhiko
Kamada, Hiroaki
Yoshida, Hiroyuki
Ishii, Ikuko
Nozawa, Eisuke
Wada, Koichi
Ugawa, Tohru
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 2018, 391 (12) : 1319 - 1326
[46] Pharmacological properties of ASP7657, a novel, potent, and selective prostaglandin EP4 receptor antagonist
Kazuhiko Mizukami
Hiroaki Kamada
Hiroyuki Yoshida
Ikuko Ishii
Eisuke Nozawa
Koichi Wada
Tohru Ugawa
Naunyn-Schmiedeberg's Archives of Pharmacology, 2018, 391 : 1319 - 1326
[47] Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold
Deng, Xinxian
Guo, Lin
Xu, Lili
Zhen, Xuechu
Yu, Kunqian
Zhao, Weili
Fu, Wei
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2015, 25 (18) : 3970 - 3974
[48] Possible involvement of the locus coeruleus in inhibition by prostanoid EP3 receptor-selective agonists of morphine withdrawal syndrome in rats
Nakagawa, T
Masuda, T
Watanabe, T
Minami, M
Satoh, M
EUROPEAN JOURNAL OF PHARMACOLOGY, 2000, 390 (03) : 257 - 266
[49] Identification and optimization of novel 1,3,4-oxadiazole EP1 receptor antagonists
Hall, Adrian
Brown, Susan H.
Chowdhury, Anita
Giblin, Gerard M. P.
Gibson, Mairi
Healy, Mark P.
Livermore, David G.
Wilson, Richard J. McArthur
Naylor, Alan
Rawlings, D. Anthony
Roman, Shilina
Ward, Emma
Willay, Caroline
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (16) : 4450 - 4455
[50] In vitro and in vivo characterization of PF-044189948, a novel, potent and selective prostaglandin EP2 receptor antagonist
af Forselles, K. J.
Root, J.
Clarke, T.
Davey, D.
Aughton, K.
Dack, K.
Pullen, N.
BRITISH JOURNAL OF PHARMACOLOGY, 2011, 164 (07) : 1847 - 1856

← 1 2 3 4 5 →