Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1

被引：39

作者：

Lorthiois, E

Bernardelli, P

Vergne, F

Oliveira, C

Mafroud, AK

Proust, E

Heuze, L

Moreau, F

Idrissi, M

Tertre, A

Bertin, B

Coupe, M

Wrigglesworth, R

Descours, A

Soulard, P

Berna, P

机构：

[1] Pfizer Global Res & Dev, F-94265 Fresnes, France

[2] 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;

D O I：

10.1016/j.bmcl.2004.07.011

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and SAR studies of spiroquinazolinones as novel PDE7 inhibitors are discussed. The best compounds from the series displayed nanomolar inhibitory affinity and were selective versus other PDE isoenzymes. (C) 2004 Elsevier Ltd. All rights reserved.

引用

收藏

页码：4623 / 4626

页数：4

相关论文

共 23 条

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

Barnes, MJ ;

Cooper, N ;

Davenport, RJ ;

Dyke, HJ ;

Galleway, FP ;

Galvin, FCA ;

Gowers, L ;

Haughan, AF ;

Lowe, C ;

Meissner, JWG ;

Montana, JG ;

Morgan, T ;

Picken, CL ;

Watson, RJ .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (08) :1081-1083

[2] CYCLIC-NUCLEOTIDE PHOSPHODIESTERASES - FUNCTIONAL IMPLICATIONS OF MULTIPLE ISOFORMS [J].

BEAVO, JA .

PHYSIOLOGICAL REVIEWS, 1995, 75 (04) :725-748

[3] CoMFA of benzyl derivatives of 2,1,3-benzo and benzothieno[3,2-a]thiadiazine 2,2-dioxides:: clues for the design of phosphodiesterase 7 inhibitors [J].

Castro, A ;

Abasolo, MI ;

Gil, C ;

Segarra, V ;

Martinez, A .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2001, 36 (04) :333-338

[4]

Conti M, 2000, PROG NUCLEIC ACID RE, V63, P1

[5]

Conti M, 2000, PRINCIPLES OF MOLECULAR REGULATION, P261

[6] INTERDEPENDENCE BETWEEN PHYSICAL PARAMETERS AND SELECTION OF SUBSTITUENT GROUPS FOR CORRELATION STUDIES [J].

CRAIG, PN .

JOURNAL OF MEDICINAL CHEMISTRY, 1971, 14 (08) :680-&

[7] Cyclic nucleotide phosphodiesterases [J].

Essayan, DM .

JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY, 2001, 108 (05) :671-680

[8]

Francis SH, 2001, PROG NUCLEIC ACID RE, V65, P1

[9]

KLUXEN FW, 2001, Patent No. 0183772

[10]

KOTERA J, 2001, PDE7 NEWS VIEWS