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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
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。
更新日期:2018-06-27
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。