Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists

被引：55

作者：

Ahn, HS ^{[1
]}

Arik, L ^{[1
]}

Boykow, G ^{[1
]}

Burnett, DA ^{[1
]}

Caplen, MA ^{[1
]}

Czarniecki, M ^{[1
]}

Domalski, MS ^{[1
]}

Foster, C ^{[1
]}

Manna, M ^{[1
]}

Stamford, AW ^{[1
]}

Wu, YS ^{[1
]}

机构：

[1] Schering Plough Corp, Res Inst, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(99)00339-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of pyrroloquinazolines has been discovered that represent novel small molecule inhibitors of the intramolecular ligand of the thrombin receptor. Analogs were prepared to study the structure-activity relationships of substitution at the N1, N3, and N7 positions of the heterocycle. Compounds 4e and 4f have been identified with IC50's of 56 and 52 nM, respectively. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：2073 / 2078

页数：6

共 50 条

[31] 3D quantitative and qualitative structure-activity relationships of the δ-opioid receptor antagonists
Chun, Sun
Lee, Jee-Young
Ro, Seong-Gu
Jeong, Ki-Woong
Kim, Yangmee
Yoon, Chang-Ju
BULLETIN OF THE KOREAN CHEMICAL SOCIETY, 2008, 29 (03): : 656 - 662
[32] Structure-activity relationships of xanthene carboxamides, novel CCR1 receptor antagonists
Naya, A
Ishikawa, M
Matsuda, K
Ohwaki, K
Saeki, T
Noguchi, K
Ohtake, N
BIOORGANIC & MEDICINAL CHEMISTRY, 2003, 11 (06) : 875 - 884
[33] STRUCTURE-ACTIVITY STUDIES OF THE THROMBIN RECEPTOR ACTIVATING PEPTIDE
SABO, T
GURWITZ, D
MOTOLA, L
BRODT, P
BARAK, R
ELHANATY, E
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1992, 188 (02) : 604 - 610
[34] Structure-activity relationships for synthetic peptide inhibitors of thrombin.
Clement, CC
Philipp, M
Gingold, J
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2003, 225 : U214 - U214
[35] Himbacine derived thrombin receptor (PAR-1) antagonists: Structure-activity relationship of the lactone ring
Xia, Yan
Chackalamannil, Samuel
Chan, Tze-Ming
Czarniecki, Michael
Doller, Dario
Eagen, Keith
Greenlee, William J.
Tsai, Hsingan
Wang, Yuguang
Ahn, Ho-Sam
Boykow, George C.
McPhail, Andrew T.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (18) : 4969 - 4972
[36] A Series of Natural Flavonoids as Thrombin Inhibitors: Structure-activity relationships
Liu, Li
Ma, Hongyue
Yang, Nianyun
Tang, Yuping
Guo, Jianming
Tao, Weiwei
Duan, Jin'ao
THROMBOSIS RESEARCH, 2010, 126 (05) : E365 - E378
[37] Synthesis and structure-activity relationships of novel P2Y2 receptor antagonists
Funke, Mario
Ko, Geun-Yung
Weyler, Stefanie
Hillmann, Petra
Hoeltje, Hans-Dieter
Mueller, Christa E.
PURINERGIC SIGNALLING, 2010, 6 (01) : 84 - 84
[38] Structure-activity relationships of a novel series of melanin-concentrating hormone (MCH) receptor antagonists
Arienzo, R
Clark, DE
Cramp, S
Daly, S
Dyke, HJ
Lockey, P
Norman, D
Roach, AG
Stuttle, K
Tomlinson, M
Wong, M
Wren, SP
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2004, 14 (15) : 4099 - 4102
[39] Synthesis and structure-activity relationships of 9-substituted acridines as endothelin-A receptor antagonists
Cheng, XM
Lee, C
Klutchko, S
Winters, T
Reynolds, EE
Welch, KM
Flynn, MA
Doherty, AM
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1996, 6 (24) : 2999 - 3002
[40] Structure-activity relationships of lysophosphatidic acid: Synthesis and analysis of Edg receptor agonists and antagonists.
Santos, WL
Heise, CE
Lynch, KR
Macdonald, TL
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2001, 222 : U687 - U687

← 1 2 3 4 5 →