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Synthesis and evaluation of new amidrazone-derived hydrazides as a potential anti-inflammatory agents.
Monatshefte für Chemie - Chemical Monthly ( IF 1.8 ) Pub Date : 2018-06-27 , DOI: 10.1007/s00706-018-2197-8
Renata Paprocka 1 , Małgorzata Wiese-Szadkowska 2 , Anna Helmin-Basa 2 , Liliana Mazur 3 , Jolanta Kutkowska 4 , Jacek Michałkiewicz 2, 5 , Bożena Modzelewska-Banachiewicz 1 , Leszek Pazderski 6
Affiliation  

Abstract

The series of new hydrazide derivatives were synthesized in reactions of N3-substituted amidrazones with cyclic anhydrides as potential anti-inflammatory and antibacterial agents. The compounds were characterized by 1H-13C two-dimensional NMR techniques, which revealed the presence of two tautomeric forms in DMSO-d6 solutions, while the molecular structure of one species was confirmed by single-crystal X-ray diffraction. The anti-inflammatory effects of hydrazides on peripheral blood mononuclear cells were experimentally evaluated. Three compounds showed antiproliferative activity comparable to ibuprofen. One derivative demonstrated strong reduction of lymphocyte proliferation stimulated by anti-CD3 antibody (by 90%) and PHA, as well as low cell toxicity. The obtained compounds exhibited relatively weak antibacterial activity; they were more effective against Gram-positive bacterial strains.

Graphical abstract



中文翻译:

新型氨基腙衍生酰肼作为潜在抗炎剂的合成和评价。

摘要

这一系列新的酰肼衍生物是在 N 3取代的脒腙与作为潜在抗炎和抗菌剂的环状酸酐的反应中合成的。化合物通过1 H- 13 C 二维 NMR 技术表征,揭示了 DMSO- d 6中存在两种互变异构体形式溶液,而一种物质的分子结构通过单晶 X 射线衍射证实。实验评价了酰肼对外周血单个核细胞的抗炎作用。三种化合物显示出与布洛芬相当的抗增殖活性。一种衍生物显示出抗 CD3 抗体 (90%) 和 PHA 刺激的淋巴细胞增殖的强烈减少,以及低细胞毒性。所得化合物的抗菌活性较弱;它们对革兰氏阳性细菌菌株更有效。

图形概要

更新日期:2018-06-27
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