Synthesis and Biological Activity of Ethyl 2-[8-Arylmethylidenehydrazino-3-Methyl-7-(1-Oxothietan-3-YL)Xanth-1-YL]Acetates

被引:1
|
作者
Gurevich, K. G. [1 ]
Urakov, A. L. [2 ]
Klen, E. E. [3 ]
Samorodov, A., V [3 ]
Nikitina, I. L. [3 ]
Khaliullin, F. A. [3 ]
Nebogatova, V. A. [3 ]
Makarova, N. N. [3 ]
Shepilova, S. O. [3 ]
Bashirova, L., I [2 ]
Khalimov, A. R. [3 ]
机构
[1] AI Evdokimov Moscow State Univ Med & Dent, 20-1 Delegatskaya St, Moscow 127473, Russia
[2] Minist Hlth RF, Izhevsk State Med Acad, 281 Kommunarov St, Izhevsk 426034, Udmurtia, Russia
[3] Bashkir State Med Univ, Minist Hlth RF, 3 Lenin St, Ufa 450008, Bashkortostan, Russia
关键词
oxothietanylxanthines; arylmethylidenehydrazines; antiplatelet; anticoagulant; antioxidant; anti-inflammatory activity; Lipinski's rule of five; DERIVATIVES;
D O I
10.1007/s11094-020-02182-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Ethyl 2-[8-Arylmethylidenehydrazino-3-methyl-7-(1-oxothietan-3-yl)xanth-1-yl]acetates (IV) were synthesized via reactions of ethyl 2-[8-hydrazino-3-methyl-7-(1-oxothietan-3-yl)xanth-1-yl]acetic acid (III) with various benzaldehydes and acetophenones. The structures of the compounds were elucidated using IR and NMR spectroscopy and elemental analysis. The antiplatelet, anticoagulation, antioxidant, and anti-inflammatory activities were assessedin vitroand in laboratory animals to identify promising compounds exhibiting antiplatelet (hydrazoneIVd) and antioxidant properties (hydrazoneIVb). BothIVbandIVdaccording toin silicocalculations were characterized by the absence of toxic risks (mutagenicity, oncogenicity, reproductive toxicity, local irritation) and had acceptable topological polar surface area so that they were promising.
引用
收藏
页码:213 / 219
页数:7
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