Synthesis and Pharmacological Activity of Ethyl-2-Amino-1-Benzamido-4-Oxo-5-(2-Oxo-2-Arylethylidene)Pyrrolidine-3-Carboxylates
- Авторлар: Zykova S.1, Darovskikh A.1, Odegova T.2, Kiselev M.2, Igidov N.2
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Мекемелер:
- Perm Federal Penal Service Institute
- Perm State Pharmaceutical Academy
- Шығарылым: Том 49, № 10 (2016)
- Беттер: 657-660
- Бөлім: Article
- URL: https://journals.rcsi.science/0091-150X/article/view/244268
- DOI: https://doi.org/10.1007/s11094-016-1347-8
- ID: 244268
Дәйексөз келтіру
Аннотация
Ethyl-2-amino-1-benzamido-4-oxo-5-(2-oxo-2-arylethylidene)pyrrolidine-3-carboxylates (IIa-g) were synthesized via recyclization of 3-(2-benzoylhydrazono)-5-arylfuran-2(3H)-ones (I) through the action of ethylcyanoacetate. The synthesized compounds were screened for biological activity and were found to have low toxicity. Ethyl-2-amino-1-benzamido-5-[2-(3, 4-dimethoxyphenyl)-2-oxoethylidene]-4-oxopyrrolidine-3-carboxylate exhibited antiradical activity in a diphenylpicrylhydrazyl (DPPH)-binding assay that was greater than that of the reference drug trolox. This same compound showed anti-inflammatory activity in a carrageenan edema model that was greater than that of diclofenac sodium. Assessment of antihypoxic activity in an acute normobaric hypoxia test found that ethyl-2-amino-1-benzamido-5-[2-oxo-2-(4-methylphenyl) ethylidene]-4-oxopyrrolidine-3-carboxylate was comparable with the succinic acid standard.
Авторлар туралы
S. Zykova
Perm Federal Penal Service Institute
Хат алмасуға жауапты Автор.
Email: zykova.sv@rambler.ru
Ресей, Ul. Karpinskogo, 125, Perm, 614012
A. Darovskikh
Perm Federal Penal Service Institute
Email: zykova.sv@rambler.ru
Ресей, Ul. Karpinskogo, 125, Perm, 614012
T. Odegova
Perm State Pharmaceutical Academy
Email: zykova.sv@rambler.ru
Ресей, Ul. Polevaya, 2, Perm, 614099
M. Kiselev
Perm State Pharmaceutical Academy
Email: zykova.sv@rambler.ru
Ресей, Ul. Polevaya, 2, Perm, 614099
N. Igidov
Perm State Pharmaceutical Academy
Email: zykova.sv@rambler.ru
Ресей, Ul. Polevaya, 2, Perm, 614099