Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Medicine and Pharmacy, 41 Victor Babes Street, RO-400010 Cluj-Napoca, Romania.
Eur J Med Chem. 2011 Feb;46(2):526-34. doi: 10.1016/j.ejmech.2010.11.032. Epub 2010 Dec 1.
This work describes recent results from our research program aiming at the synthesis and evaluation of new compounds acting as potential anti-inflammatory drugs. A series of novel acyl-hydrazones bearing 2-aryl-thiazole moiety were synthesized by the condensation between derivatives of 4-[2-(4-methyl-2-phenyl-thiazole-5-yl)-2-oxo-ethoxy]-benzaldehyde and 2, 3 or 4-(2-aryl-thiazol-4-ylmethoxy)-benzaldehyde, respectively and different carboxylic acid hydrazides. The structures of newly synthesized compounds were established by the combined use of IR, (1)H NMR, mass spectral data and elemental analysis. These compounds were tested in vivo for their anti-inflammatory activity, in an acute experimental inflammation. The acute phase bone marrow response, phagocytes' activity and NO synthesis were evaluated. Compounds 10, 15, 17, 18 and 22 reduced the absolute leukocytes count due to the lower neutrophils percentage. Phagocitary index was decreased by all the compounds. Seven of them reduced the phagocitary activity. Five compounds inhibited NO synthesis, 3, 4, 16 and 22 stronger than Meloxicam, the anti-inflammatory reference drug.
这项工作描述了我们的研究计划的最新结果，该计划旨在合成和评估新的化合物，这些化合物作为潜在的抗炎药物。通过将 4-[2-(4-甲基-2-苯基-噻唑-5-基)-2-氧代乙氧基]-苯甲醛衍生物与 2,3 或 4-(2-苯基-噻唑-4-基甲氧基)-苯甲醛和不同羧酸酰肼缩合，合成了一系列含有 2-芳基噻唑部分的新型酰腙。新合成化合物的结构通过红外光谱（IR）、（1）H NMR、质谱数据和元素分析的综合使用来确定。这些化合物在体内进行了抗炎活性测试，在急性实验性炎症中进行了测试。评估了急性骨髓反应、吞噬细胞活性和 NO 合成。化合物 10、15、17、18 和 22 由于中性粒细胞百分比降低而降低了绝对白细胞计数。吞噬指数被所有化合物降低。其中 7 种降低了吞噬细胞的活性。有 5 种化合物抑制了 NO 的合成，其中 3、4、16 和 22 比抗炎参考药物美洛昔康更强。
