Syntheses and evaluation of pyrido[2,3-d]pyrimidine-2,4-diones as PDE 4 inhibitors

被引:40
作者
Nam, G
Yoon, CM
Kim, E
Rhee, CK
Kim, JH
Shin, JH
Kim, SH
机构
[1] Korea Inst Sci & Technol, Biochem Res Ctr, Seoul 130650, South Korea
[2] Korea Univ, Coll Sci & Technol, Dept Chem, Chungnam 339700, South Korea
[3] Cheiljedang Corp, Kyonggi Do 467810, South Korea
[4] Seoul Natl Univ, Sch Chem & Mol Engn, Seoul 151742, South Korea
关键词
D O I
10.1016/S0960-894X(00)00681-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The syntheses and in vitro evaluation of a new series of pyrido[2,3-d]pyrimidine-2,4-diones bearing substituents at C-3 and/or C-4 positions on the pyridine ring are described. Some of these compounds, especially 51 and 6f, were found to be potent phosphodiesterase 4 (PDE 4) inhibitors exhibiting improved ratio of PDE 4 inhibitory activity:rolipram binding assay (RBA). (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:611 / 614
页数:4
相关论文
共 19 条
[1]  
Alvarez R., 1994, CAN J PHYSL PHARM S1, V72, P510
[2]   1,4-cyclohexanecarboxylates: Potent and selective inhibitors of phosphodiesterase 4 for the treatment of asthma [J].
Christensen, SB ;
Guider, A ;
Forster, CJ ;
Gleason, JG ;
Bender, PE ;
Karpinski, JM ;
DeWolf, WE ;
Barnette, MS ;
Underwood, DC ;
Griswold, DE ;
Cieslinski, LB ;
Burman, M ;
Bochnowicz, S ;
Osborn, RR ;
Manning, CD ;
Grous, M ;
Hillegas, LM ;
Bartus, JO ;
Ryan, MD ;
Eggleston, DS ;
Haltiwanger, RC ;
Torphy, TJ .
JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (06) :821-835
[3]   Phosphodiesterase 4 inhibitors, structurally unrelated to Rolipram, as promising agents for the treatment of asthma and other pathologies [J].
Dal Piaz, V ;
Giovannoni, MP .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2000, 35 (05) :463-480
[4]   Phosphodiesterase 4 inhibitors as novel anti-inflammatory agents [J].
Doherty, AM .
CURRENT OPINION IN CHEMICAL BIOLOGY, 1999, 3 (04) :466-473
[5]  
LOMBARDO LJ, 1995, CURR PHARM DESIGN, V1, P255
[6]   STRUCTURE ACTIVITY RELATIONSHIP OF QUINAZOLINEDIONE INHIBITORS OF CALCIUM-INDEPENDENT PHOSPHODIESTERASE [J].
LOWE, JA ;
ARCHER, RL ;
CHAPIN, DS ;
CHENG, JB ;
HELWEG, D ;
JOHNSON, JL ;
KOE, BK ;
LEBEL, LA ;
MOORE, PF ;
NIELSEN, JA ;
RUSSO, LL ;
SHIRLEY, JT .
JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (02) :624-628
[7]  
MARK A, 2000, DRUGS, V59, P193
[8]  
NORMAN P, 1998, DRUGS FUTURE, V23, P607
[9]  
NORMAN P, 1998, EXERT OPIN THER PAT, V8, P1529
[10]  
PALFREYMAN MN, 1996, PROGR MED CHEM, P1