Tozkoparan Birsen, Gökhan Nesrin, Küpeli Esra, Yeşilada Erdem, Ertan Mevlüt
Hacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Chemistrya, Sihhiye, Ankara, Turkey.
Arzneimittelforschung. 2004;54(1):35-41. doi: 10.1055/s-0031-1296934.
A series of 6-(alpha-amino-4-chlorobenzyl)-thiazolo[3,2-b]-1,2,4-triazol-5-ols (2a-j) were synthesized from 6-(4-chlorobenzylidene) thiazolo[3,2-b]-1,2,4-triazolo-5(6H)-one (2) by applying Michael addition reaction. All the compounds were characterized by their melting points, elementary analysis, IR and 1H-NMR spectra and screened for their anti-inflammatory and analgesic activities. Among the derivatives compound 2i bearing 4-(4-acetylphenyl)piperazine showed the highest and dose-dependent analgesic and anti-inflammatory activity without inducing any gastric lesion.
通过迈克尔加成反应,由6-(4-氯亚苄基)噻唑并[3,2-b]-1,2,4-三唑-5(6H)-酮(2)合成了一系列6-(α-氨基-4-氯苄基)-噻唑并[3,2-b]-1,2,4-三唑-5-醇(2a-j)。所有化合物均通过熔点、元素分析、红外光谱和1H-核磁共振光谱进行表征,并对其抗炎和镇痛活性进行筛选。在这些衍生物中,带有4-(4-乙酰苯基)哌嗪的化合物2i表现出最高的剂量依赖性镇痛和抗炎活性,且未引起任何胃部损伤。