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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 19期

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

页码：2235 / 2238

页数：4

共 18 条

[1] SELECTIVE TYPE-IV PHOSPHODIESTERASE INHIBITORS AS ANTIASTHMATIC AGENTS - THE SYNTHESES AND BIOLOGICAL-ACTIVITIES OF 3-(CYCLOPENTYLOXY)-4-METHOXYBENZAMIDES AND ANALOGS [J].

ASHTON, MJ ;

COOK, DC ;

FENTON, G ;

KARLSSON, JA ;

PALFREYMAN, MN ;

RAEBURN, D ;

RATCLIFFE, AJ ;

SOUNESS, JE ;

THURAIRATNAM, S ;

VICKER, N .

JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (11) :1696-1703

[2]

Barnette MS, 1996, BIOCHEM PHARMACOL, V51, P949

[3]

BARNETTE MS, 1995, J PHARMACOL EXP THER, V273, P1396

[4]

BRUNCE KT, 1976, J PHYSL, P453

[5] SYNTHESIS AND IN-VITRO PROFILE OF A NOVEL SERIES OF CATECHOL BENZIMIDAZOLES - THE DISCOVERY OF POTENT, SELECTIVE PHOSPHODIESTERASE TYPE-IV INHIBITORS WITH GREATLY ATTENUATED AFFINITY FOR THE [H-3] ROLIPRAM BINDING-SITE [J].

CHENG, JB ;

COOPER, K ;

DUPLANTIER, AJ ;

EGGLER, JF ;

KRAUS, KG ;

MARSHALL, SC ;

MARFAT, A ;

MASAMUNE, H ;

SHIRLEY, JT ;

TICKNER, JE ;

UMLAND, JP .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1995, 5 (17) :1969-1972

[6] 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

[7]

DAVIDSEN SK, 1995, EXPERT OPIN THER PAT, V5, P1087

[8]

Dyke H J, 1999, Expert Opin Investig Drugs, V8, P1301, DOI 10.1517/13543784.8.9.1301

[9] The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I [J].

Hulme, C ;

Moriarty, K ;

Miller, B ;

Mathew, R ;

Ramanjulu, M ;

Cox, P ;

Souness, J ;

Page, KM ;

Uhl, J ;

Travis, J ;

Huang, FC ;

Labaudiniere, R ;

Djuric, SW .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (14) :1867-1872

[10]

HULME C, 1988, BIOORG MED CHEM LETT, V8, P3053

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