Synthesis of ibuprofen heterocyclic amides and investigation of their analgesic and toxicological properties

被引：73

作者：

Cocco, MT ^{[1
]}

Congiu, C ^{[1
]}

Onnis, V ^{[1
]}

Morelli, M ^{[1
]}

Cauli, O ^{[1
]}

机构：

[1] Univ Cagliari, Dipartimento Tossicol, I-09124 Cagliari, Italy

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 38卷 / 05期

关键词：

ibuprofen amides; analgesic activity; ulcerogenic activity; aminopyridine; aminopyrimidine;

D O I：

10.1016/S0223-5234(03)00074-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of amides of ibuprofen with heteroaromatic amines was synthesized and assayed in vivo for their analgesic properties by means of writhing test in rats. When compared to parent ibuprofen some of the new amides exhibited a comparable or improved analgesic activity and a lower ulcerogenic effect. (C) 2003 Editions scientificlues et medicales Elsevier SAS. All rights reserved.

引用

页码：513 / 518

页数：6

共 53 条

[1] Chloropyrimidines as a new class of antimicrobial agents [J].

Agarwal, N ;

Srivastava, P ;

Raghuwanshi, SK ;

Upadhyay, DN ;

Sinha, S ;

Shukla, PK ;

Ram, VJ .

BIOORGANIC & MEDICINAL CHEMISTRY, 2002, 10 (04) :869-874

[2]

Akgun H, 1996, ARZNEIMITTEL-FORSCH, V46, P891

[3] Design and synthesis of novel antibacterial agents with inhibitory activity against DNA polymerase III [J].

Ali, A ;

Aster, SD ;

Graham, DW ;

Patel, GF ;

Taylor, GE ;

Tolman, RL ;

Painter, RE ;

Silver, LL ;

Young, K ;

Ellsworth, K ;

Geissler, W ;

Harris, GS .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (16) :2185-2188

[4] GASTROINTESTINAL DAMAGE ASSOCIATED WITH THE USE OF NONSTEROIDAL ANTIINFLAMMATORY DRUGS [J].

ALLISON, MC ;

HOWATSON, AG ;

TORRANCE, CJ ;

LEE, FD ;

RUSSELL, RI .

NEW ENGLAND JOURNAL OF MEDICINE, 1992, 327 (11) :749-754

[5]

[Anonymous], 1996, CANC PAIN REL GUID O

[6]

ARNOLD JD, 1986, Patent No. 4587252

[7]

ARNOLD JD, 1986, Patent No. 4571400

[8]

BAKER GL, 1986, Patent No. 4569937

[9]

Bakhite EA, 2000, PHARMAZIE, V55, P577

[10]

BANG H, 1998, Patent No. 9847502

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