Synthesis and Antiglycating Activity of 2-Aminopropylmorpholino-5-Aryl-6H-1,3,4-Thiadiazine Dihydrobromides and 2-Aminopropylmopholino-5-Thienyl-6H-1,3,4-Thiadiazine Dihydrobromides

被引：0
|
作者：
T. A. Tseitler
L. P. Sidorova
V. V. Emel’yanov
E. A. Savateeva
O. N. Chupakhin
机构：
[1] Urals First President of Russian B. N. Yeltsin Federal University,I. Ya. Postovskii Institute of Organic Synthesis
[2] Urals Branch,undefined
[3] Russian Academy of Sciences,undefined
来源：
Pharmaceutical Chemistry Journal | 2020年 / 53卷
关键词：
1,3,4-thiadiazine; cyclocondensation; α-haloacetophenones; α-haloacetylthiophenones; non-enzymatic protein glycation;
D O I：
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中图分类号：
学科分类号：
摘要：
A group of novel 2-propylmorpholino-5-aryl- and 5-thienyl-6H-1,3,4-thiadiazine dihydrobromides was synthesized by cyclocondensation of 4-[3-(4-morpholino)propyl]-3-thiosemicarbazide with α –haloacetoarenones or α-haloacetylthiophenones. Two compounds of this group were found to produce effective inhibition of non-enzymatic protein glycation in an in vitro model system. These test results indicate that compounds IIIa and IIIc, which contain phenyl- and 4′ -chlorophenyl groups at position 5 of the thiadiazine ring respectively, are candidates for in vivo studies.
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页码：890 / 894
页数：4
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