Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: Design, synthesis and structure-activity relationship studies

被引：49

作者：

Vergne, F

Bernardelli, P

Lorthiois, E

Pham, N

Proust, E

Oliveira, C

Mafroud, AK

Royer, F

Wrigglesworth, R

Schellhaas, JK

Barvian, MR

Moreau, F

Idrissi, M

Tertre, A

Bertin, B

Coupe, M

Berna, P

Soulard, P

机构：

[1] Pfizer Global Res & Dev, F-92465 Fresnes, France

[2] Pfizer Global Res & Dev, Ann Arbor Labs, Ann Arbor, MI 48105 USA

[3] Pfizer Discovery Technol Ctr, Cambridge, MA 02139 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 18期

关键词：

PDE7; phosphodiesterase; cAMP;

D O I：

10.1016/j.bmcl.2004.07.008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and SAR studies of a series of structurally novel small molecule inhibitors of PDE7 are discussed. The best compounds from the series displayed low nanomolar inhibitory activity and are selective versus PDE4. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：4607 / 4613

页数：7

共 28 条

[1] Synthesis and structure-activity relationships of guan analogues as phosphodiesterase 7 (PDE7) inhibitors [J].