一些 N-吡啶基-N'-噻唑基腙衍生物的合成与抗结核活性。

Synthesis and antituberculosis activity of some N-pyridyl-N'-thiazolylhydrazine derivatives.

机构信息

Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 26470 Eskişehir, Turkey.

出版信息

Eur J Med Chem. 2010 May;45(5):2085-8. doi: 10.1016/j.ejmech.2010.01.017. Epub 2010 Jan 20.

DOI:10.1016/j.ejmech.2010.01.017

PMID:20149489

Abstract

In this study, new N-(1-arylethylidene)-N'-(4-arylthiazol-2-yl)hydrazine derivatives were synthesized and evaluated for their antituberculosis activity. The chemical structures of the compounds were elucidated by IR, NMR and FAB+-MS spectral data and Elemental Analyses. The initial screen was conducted against Mycobacterium tuberculosis H37Rv (ATCC 27294) in BACTEC 12B medium using the Microplate Alamar Blue Assay (MABA). The VERO cell cytotoxicity assay was done in parallel with the TB Dose Response assay. Viability was assessed using Promega's Cell Titer-Glo Luminescent Cell Viability Assay. Cytotoxicity was determined from the dose-response curve as the CC50 using a curve-fitting program. One of the compounds showed high activity with low toxicity.

摘要

在这项研究中，合成了新型 N-(1-芳基亚乙基)-N'-(4-芳基噻唑-2-基)腙衍生物，并评估了它们的抗结核活性。通过 IR、NMR 和 FAB+-MS 光谱数据和元素分析阐明了化合物的化学结构。初步筛选是在 BACTEC 12B 培养基中使用微孔板 Alamar 蓝测定法 (MABA) 对结核分枝杆菌 H37Rv (ATCC 27294) 进行的。与 TB 剂量反应测定平行进行了 VERO 细胞细胞毒性测定。使用 Promega 的 Cell Titer-Glo 发光细胞活力测定法评估活力。通过曲线拟合程序，从剂量反应曲线中确定了细胞毒性作为 CC50。其中一种化合物表现出高活性和低毒性。