학술논문

Synthesis and Pharmacological Activity of Ethyl-2-Amino-1-Benzamido-4-Oxo-5-(2-Oxo-2-Arylethylidene)Pyrrolidine-3-Carboxylates.
Document Type
Article
Source
Pharmaceutical Chemistry Journal. Jan2016, Vol. 49 Issue 10, p657-660. 4p.
Subject
*PYRROLIDINE derivatives
*CHEMICAL synthesis
*CARBOXYLATES
*DICLOFENAC
*SUCCINIC acid
*PHARMACEUTICAL chemistry
Language
ISSN
0091-150X
Abstract
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(3 H)-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. [ABSTRACT FROM AUTHOR]