The synthesis and biological evaluation of a novel series of phthalazine PDE4 inhibitors I

被引:45
作者
Napoletano, M
Norcini, G
Pellacini, F
Marchini, F
Morazzoni, G
Ferlenga, P
Pradella, L
机构
[1] Zambon Grp, Inpharzam Ric, CH-6814 Cadempino, Switzerland
[2] Zambon Grp SpA, R&D, I-20091 Milan, Italy
关键词
D O I
10.1016/S0960-894X(00)00449-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
This communication describes the synthesis and in vitro evaluation of a novel and potent series of phosphodiesterase type IV (PDE4) inhibitors. The compounds described represent conformationally constrained analogues of RP 73401, Piclamilast. Preliminary evidences of reduced side effects of 11 compared to standards are also reported. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2235 / 2238
页数:4
相关论文
共 18 条
[11]   INHIBITION OF CYCLIC ADENOSINE-3',5'-MONOPHOSPHATE PHOSPHODIESTERASE FROM VASCULAR SMOOTH-MUSCLE BY ROLIPRAM ANALOGS [J].
MARIVET, MC ;
BOURGUIGNON, JJ ;
LUGNIER, C ;
MANN, A ;
STOCLET, JC ;
WERMUTH, CG .
JOURNAL OF MEDICINAL CHEMISTRY, 1989, 32 (07) :1450-1457
[12]   EFFECTS OF SELECTIVE PHOSPHODIESTERASE INHIBITORS ON THE POLYMORPHONUCLEAR LEUKOCYTE RESPIRATORY BURST [J].
NIELSON, CP ;
VESTAL, RE ;
STURM, RJ ;
HEASLIP, R .
JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY, 1990, 86 (05) :801-808
[13]  
Palfreyman M N, 1996, Prog Med Chem, V33, P1, DOI 10.1016/S0079-6468(08)70302-3
[14]  
REGAN G, 1988, BIOORG MED CHEM LETT, V8, P2737
[15]   CLOSE CORRELATION BETWEEN BEHAVIORAL-RESPONSE AND BINDING INVIVO FOR INHIBITORS OF THE ROLIPRAM-SENSITIVE PHOSPHODIESTERASE [J].
SCHMIECHEN, R ;
SCHNEIDER, HH ;
WACHTEL, H .
PSYCHOPHARMACOLOGY, 1990, 102 (01) :17-20
[16]   STEREOSPECIFIC BINDING OF THE ANTIDEPRESSANT ROLIPRAM TO BRAIN PROTEIN STRUCTURES [J].
SCHNEIDER, HH ;
SCHMIECHEN, R ;
BREZINSKI, M ;
SEIDLER, J .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1986, 127 (1-2) :105-115
[17]  
Stafford Jeffrey A., 1996, V31, P71
[18]   Phosphodiesterase isozymes - Molecular targets for novel antiasthma agents [J].
Torphy, TJ .
AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE, 1998, 157 (02) :351-370