Synthesis and Analgesic Activity of 4,10-Bis((±)-5-Benzoyl-2,3-Dihydro-1hpyrrolo[1,2-a]Pyrrole-1-Carbonyl)-2,6,8,12-Tetraacetyl-2,4,6,8,10,12-Hexaazatetracyclo[5,5,03,11,05,9]Dodecane

被引:2
作者
Kulagina, D. A. [1 ]
Sysolyatin, S. V. [1 ]
Kalashnikov, A. I. [1 ]
Malykhin, V. V. [1 ]
Sonina, E. G. [1 ]
Shevchenko, A. V. [1 ]
Krylova, S. G. [2 ]
Lopatina, K. A. [2 ]
Zueva, E. P. [2 ]
Razina, T. G. [2 ]
Rybalkina, O. Yu. [2 ]
Amosova, E. N. [2 ]
机构
[1] Russian Acad Sci, Inst Problems Chem & Energy Technol, Siberian Branch, 1 Sotsialist Skaya St, Biisk 659322, Russia
[2] Russian Acad Sci, ED Goldberg Sci Res Inst Pharmacol & Regenerat Me, Tomsk Natl Med Res Ctr, 3 Lenin Prospekt, Tomsk 634028, Russia
关键词
framework amines; analgesic activity;
D O I
10.1007/s11094-021-02332-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A method of preparing the potential analgesic substance 4,10-bis((+/-)-5-benzoyl-2,3-dihydro-1H-pyrrolo-[1,2-a]pyrrole-1-carbonyl)-2,6,8,12-tetraacetyl-2,4,6,8,10,12-hexaazatetracyclo[5,5,0(3,11),0(5,9)]dodecane is described in detail. Different conditions for preparing the target substance are considered and its full physicochemical properties are presented. Marked analgesic activity of this innovatory compound was found in conditions of thermal nociception in the hotplate test and acute visceral and somatic deep pain in the acetic writhings test.
引用
收藏
页码:1140 / 1144
页数:5
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