Synthesis and SAR of 2-(4-fluorophenyl)-3-pyrimidin-4-ylimidazo[1,2-a]pyridine derivatives as anticoccidial agents

被引：19

作者：

Feng, Dennis

Fisher, Michael

Liang, Gui-Bai

Qian, Xiaoxia

Brown, Chris

Gurnett, Anne

Leavitt, Penny Sue

Liberator, Paul A.

Mathew, John

Misura, Andrew

Samaras, Samantha

Tamas, Tamas

Schmatz, Dennis M.

Wyvratt, Matthew

Biftu, Tesfaye

机构：

[1] Merck & Co Inc, Dept Med Chem, Merck Res Labs, Rahway, NJ 07065 USA

[2] Merck & Co Inc, Human & Anim Infect Dis Res, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 23期

关键词：

kinase; coccidiosis; parasite; imidazopyrimidine; PKG inhibitor;

D O I：

10.1016/j.bmcl.2006.08.127

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Compounds 10a-10d and 10i are very potent inhibitors of Eimeria tenella cGMP-dependent protein kinase (0.081-0.32 nM) and are very efficacious antiparasitic agents in vivo when administered to chickens at 12.5-25 ppm levels in the feed. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：5978 / 5981

页数：4

共 6 条

[1] Synthesis and SAR studies of very potent imidazopyridine antiprotozoal agents
Biftu, T
Feng, D
Fisher, M
Liang, GB
Qian, XX
Scribner, A
Dennis, R
Lee, S
Liberator, PA
Brown, C
Gurnett, A
Leavitt, PS
Thompson, D
Mathew, J
Misura, A
Samaras, S
Tamas, T
Sina, JF
McNulty, KA
McKnight, CG
Schmatz, DM
Wyvratt, M
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (09) : 2479 - 2483
[2] Synthesis and SAR of 2,3-diarylpyrrole inhibitors of parasite cGMP-dependent protein kinase as novel anticoccidial agents
Biftu, T
Feng, D
Ponpipom, M
Girotra, N
Liang, GB
Qian, XX
Bugianesi, R
Simeone, J
Chang, L
Gurnett, A
Liberator, P
Dulski, P
Leavitt, PS
Crumley, T
Misura, A
Murphy, T
Rattray, S
Samaras, S
Tamas, T
Mathew, J
Brown, C
Thompson, D
Schmatz, D
Fisher, M
Wyvratt, M
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (13) : 3296 - 3301
[3] BIFTU T, Patent No. 20040176396
[4] Toxoplasma gondii cyclic GMP-dependent kinase:: Chemotherapeutic targeting of an essential parasite protein kinase
Donald, RGK
Allocco, J
Singh, SB
Nare, B
Salowe, SP
Wiltsie, J
Liberator, PA
[J]. EUKARYOTIC CELL, 2002, 1 (03) : 317 - 328
[5] Purification and molecular characterization of cGMP-dependent protein kinase from apicomplexan parasites - A novel chemotherapeutic target
Gurnett, AM
Liberator, PA
Dulski, PM
Salowe, SP
Donald, RGK
Anderson, JW
Wiltsie, J
Diaz, CA
Harris, G
Chang, B
Darkin-Rattray, SJ
Nare, B
Crumley, T
Blum, PS
Misura, AS
Tamas, T
Sardana, MK
Yuan, J
Biftu, T
Schmatz, DM
[J]. JOURNAL OF BIOLOGICAL CHEMISTRY, 2002, 277 (18) : 15913 - 15922
[6] Tamas T., 1994, Poultry Science, V73, P15

← 1 →