Medicinal chemistry of N-acylhydrazones: Novel lead-compounds of analgesic, antinflammatory and antithrombotic drugs.

被引：59

作者：

Barreiro, EJ ^{[1
]}

Fraga, CAM ^{[1
]}

Miranda, ALP ^{[1
]}

Rodrigues, CR ^{[1
]}

机构：

[1] Univ Fed Rio de Janeiro, Fac Farm, LASSBio, BR-21944190 Rio De Janeiro, Brazil

来源：

QUIMICA NOVA | 2002年 / 25卷 / 01期

关键词：

bioactive N-acythydrazones derivatives; antinflammatory; analgesic and antithrombotic properties; molecular hybridization and bioisosterism in drug; design;

D O I：

10.1590/S0100-40422002000100022

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

In this article are described new bioactive N-acylhydrazone (NAH) derivatives, structurally designed as optimization or aryl hydrazones precursors planned by molecular hybridization of two 5-lipoxigenase inhibitors, e,g. CBS-1108 and BW-755c. The analgesic, antiedematogenic and anti-platelet aggregating profile of several isosteric compounds was investigated by using classic pharmacological assays in vivo and ex-vivo, allowing to identify new potent peripheric analgesic lead, a new anti-inflammatory and an antithrombotic agent. During this study was discovered dozen of active NAH compound, clarifying the structure-activity relationship for this series of NAH derivatives, indicating the pharmacophore character of the N-acylhydrazone functionality.

引用

页码：129 / 148

页数：20

共 125 条

[71]

Lima L M, 1999, Pharm Acta Helv, V73, P281, DOI 10.1016/S0031-6865(99)00004-7

[72]

Lima Lidia M., 1999, Pharmacy and Pharmacology Communications, V5, P673

[73] O-alkylation of bioactive phthalimide derivatives under microwave irradiation in dry media [J].

Lima, LM ;

Barreiro, EJ ;

Fraga, CAM .

SYNTHETIC COMMUNICATIONS, 2000, 30 (18) :3291-3306

[74] Synthesis and analgesic activity of novel N-acylarylhydrazones and isosters, derived from natural safrole [J].

Lima, PC ;

Lima, LM ;

da Silva, KCM ;

Léda, PHO ;

de Miranda, ALP ;

Fraga, CAM ;

Barreiro, EJ .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2000, 35 (02) :187-203

[75] PHENYLHYDRAZONES AS NEW GOOD SUBSTRATES FOR THE DIOXYGENASE AND PEROXIDASE REACTIONS OF PROSTAGLANDIN SYNTHASE - FORMATION OF IRON(III)-SIGMA-PHENYL COMPLEXES [J].

MAHY, JP ;

GASPARD, S ;

MANSUY, D .

BIOCHEMISTRY, 1993, 32 (15) :4014-4021

[76] Design of selective inhibitors of cyclooxygenase-2 as nonulcerogenic anti-inflammatory agents [J].

Marnett, LJ ;

Kalgutkar, AS .

CURRENT OPINION IN CHEMICAL BIOLOGY, 1998, 2 (04) :482-490

[77]

MARTINS RCA, 1995, THESIS

[78]

MATHEUS ME, 1991, BRAZ J MED BIOL RES, V24, P1219

[79]

Miranda A. L. P., 1994, CAN J PHYSL PHARM S1, V72, P210

[80]

MONTEIRO TM, 1993, THESIS

← 3 4 5 6 7 8 9 10 11 12 →