Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors

被引:41
作者
Yin, Yan [1 ,2 ]
Lin, Li [1 ,2 ]
Ruiz, Claudia [1 ,2 ]
Cameron, Michael D. [1 ,2 ]
Pocas, Jennifer [1 ,2 ]
Grant, Wayne [1 ,2 ]
Schroeter, Thomas [1 ,2 ]
Chen, Weimin [1 ,2 ]
Duckett, Derek [1 ,2 ]
Schuerer, Stephan [3 ,4 ]
LoGrasso, Philip [1 ,2 ]
Feng, Yangbo [1 ,2 ]
机构
[1] Scripps Res Inst, Translat Res Inst, Jupiter, FL 33458 USA
[2] Scripps Res Inst, Dept Mol Therapeut, Jupiter, FL 33458 USA
[3] Univ Miami, Dept Pharmacol, Miami, FL 33136 USA
[4] Univ Miami, Ctr Computat Sci, Miami, FL 33136 USA
关键词
ROCK; Rho; Benzothiazole; Chroman; Pyrazole; Glaucoma; INTRAOCULAR-PRESSURE; PROTEIN-KINASE; SMOOTH-MUSCLE; DESIGN; POTENT; HYPERTENSION; DISCOVERY; FASUDIL; TARGET; MODEL;
D O I
10.1016/j.bmcl.2009.09.115
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of benzothiazole derivatives as ROCK inhibitors have been discovered. Compounds with good biochemical and cellular potency, and sufficient kinase selectivity have been identified. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码:6686 / 6690
页数:5
相关论文
共 28 条
[1]   Chroman-3-amides as potent Rho kinase inhibitors [J].
Chen, Yen Ting ;
Bannister, Thomas D. ;
Weiser, Amiee ;
Griffin, Evelyn ;
Lin, Li ;
Ruiz, Claudia ;
Cameron, Michael D. ;
Schurer, Stephan ;
Duckett, Derek ;
Schroter, Thomas ;
LoGrasso, Philip ;
Feng, Yangbo .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (24) :6406-6409
[2]   Discovery of Substituted 4-(Pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as Potent and Highly Selective Rho Kinase (ROCK-II) Inhibitors [J].
Feng, Yangbo ;
Yin, Yan ;
Weiser, Arniee ;
Griffin, Evelyn ;
Cameron, Michael D. ;
Lin, Li ;
Ruiz, Claudia ;
Schuerer, Stephan C. ;
Inoue, Toshihiro ;
Rao, P. Vasanth ;
Schroeter, Thomas ;
LoGrasso, Philip .
JOURNAL OF MEDICINAL CHEMISTRY, 2008, 51 (21) :6642-6645
[3]   Structure-activity relationships, and drug metabolism and pharmacokinetic properties for indazole piperazine and indazole piperidine inhibitors of ROCK-II [J].
Feng, Yangbo ;
Cameron, Michael D. ;
Frackowiak, Bozena ;
Griffin, Evelyn ;
Lin, Li ;
Ruiz, Claudia ;
Schroter, Thomas ;
LoGrasso, Philip .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (08) :2355-2360
[4]   The Effect of the Rho-Associated Protein Kinase Inhibitor, HA-1077, in the Rabbit Ocular Hypertension Model Induced by Water Loading [J].
Fukunaga, Takaki ;
Ikesugi, Kengo ;
Nishio, Masahiro ;
Sugimoto, Masahiko ;
Sasoh, Mikio ;
Hidaka, Hiroyoshi ;
Uji, Yukitaka .
CURRENT EYE RESEARCH, 2009, 34 (01) :42-47
[5]   Synthesis and evaluation of 4-(1-aminoalkyl)-N-(4-pyridyl)cyclohexanecarboxamides as Rho kinase inhibitors and neurite outgrowth promoters [J].
Gingras, K ;
Avedissian, H ;
Thouin, E ;
Boulanger, W ;
Essagian, C ;
McKerracher, L ;
Lubell, WD .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2004, 14 (19) :4931-4934
[6]   Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors [J].
Goodman, Krista B. ;
Cui, Haifeng ;
Dowdell, Sarah E. ;
Gaitanopoulos, Dimitri E. ;
Ivy, Robert L. ;
Sehon, Clark A. ;
Stavenger, Robert A. ;
Wang, Gren Z. ;
Viet, Andrew Q. ;
Xu, Weiwei ;
Ye, Guosen ;
Semus, Simon F. ;
Evans, Christopher ;
Fries, Harvey E. ;
Jolivette, Larry J. ;
Kirkpatrick, Robert B. ;
Dul, Edward ;
Khandekar, Sanjay S. ;
Yi, Tracey ;
Jung, David K. ;
Wright, Lois L. ;
Smith, Gary K. ;
Behm, David J. ;
Bentley, Ross ;
Doe, Christopher P. ;
Hu, Erding ;
Lee, Dennis .
JOURNAL OF MEDICINAL CHEMISTRY, 2007, 50 (01) :6-9
[7]   Rho-kinase as a drug target for the treatment of airway hyperresponsiveness in asthma [J].
Gosens, R ;
Schaafsma, D ;
Nelemans, SA ;
Halayko, AJ .
MINI-REVIEWS IN MEDICINAL CHEMISTRY, 2006, 6 (03) :339-348
[8]   Design and synthesis of rho kinase inhibitors (III) [J].
Iwakubo, Masayuki ;
Takami, Atsuya ;
Okada, Yuji ;
Kawata, Takehisa ;
Tagami, Yoshimichi ;
Sato, Motoko ;
Sugiyama, Terumi ;
Fukushima, Kayoko ;
Taya, Shinichiro ;
Amano, Mutsuki ;
Kaibuchi, Kozo ;
Iijima, Hiroshi .
BIOORGANIC & MEDICINAL CHEMISTRY, 2007, 15 (02) :1022-1033
[9]   Design and synthesis of Rho kinase inhibitors (II) [J].
Iwakubo, Masayuki ;
Takami, Atsuya ;
Okada, Yuji ;
Kawata, Takehisa ;
Tagami, Yoshimichi ;
Ohashi, Hiroshi ;
Sato, Motoko ;
Sugiyama, Terumi ;
Fukushima, Kayoko ;
Iijima, Hiroshi .
BIOORGANIC & MEDICINAL CHEMISTRY, 2007, 15 (01) :350-364
[10]  
Leung T, 1996, MOL CELL BIOL, V16, P5313