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 3 条

[1] Medicinal chemistry of N-acylhydrazones: New lead-compounds of analgesic, antiinflammatory and antithrombotic drugs
Fraga, CAM
Barreiro, EJ
CURRENT MEDICINAL CHEMISTRY, 2006, 13 (02) : 167 - 198
[2] Design, synthesis and analgesic properties of novel conformationally-restricted N-acylhydrazones (NAH)
Kuemmerle, Arthur E.
Vieira, Marina M.
Schmitt, Martine
Miranda, Ana L. P.
Fraga, Carlos A. M.
Bourguignon, Jean-Jacques
Barreiro, Eliezer J.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (17) : 4963 - 4966
[3] Design, Synthesis, and Pharmacological Evaluation of N-Acylhydrazones and Novel Conformationally Constrained Compounds as Selective and Potent Orally Active Phosphodiesterase-4 Inhibitors
Kuemmerle, Arthur E.
Schmitt, Martine
Cardozo, Suzana V. S.
Lugnier, Claire
Villa, Pascal
Lopes, Alexandra B.
Romeiro, Nelilma C.
Justiniano, Helene
Martins, Marco A.
Fraga, Carlos A. M.
Bourguignon, Jean-Jacques
Barreiro, Eliezer J.
JOURNAL OF MEDICINAL CHEMISTRY, 2012, 55 (17) : 7525 - 7545

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