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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and Biological Activity of 4-Amino-1-Methyl-5-Imidazolecarboxylic Acid Derivatives

Author(s): A. Regiec, H. Mastalarz, R. Miedzybrodzki, K. Smietanska and R. Jasztold-Howorko

Volume 3 , Issue 3 , 2006

Page: [192 - 199] Pages: 8

DOI: 10.2174/157018006776286961

Price: $65


The main goal of our study was the synthesis and biological evaluation of 4-amino- and 4-[(4- chlorobenzoyl)amino]-1-methylimidazole N-substituted 5-carboxamides. Biological in vitro tests indicated their remarkable influence on some cellular immune and inflammatory responses compared with ibuprofen and leflunomide as reference drugs. The toxicity of the tested compounds on murine bone marrow cells was also determined. The anti-inflammatory activity of 4-[(4-chlorobenzoyl)amino]-5-[N-(4-chlorophenyl)]-1-methyl- 5-imidazolecarboxamide (7a) was confirmed in vivo in the carrageenan-induced oedema test. Comparison of the biological activity of 7a with that of the isosteric isothiazole derivative MR-2/94 suggests that replacement of the isothiazole core ring system with an imidazole one resulted in a considerable lowering of toxicity while maintaining anti-inflammatory and immunotropic properties.

Keywords: Imidazoles, anti-inflammatory, nitric oxide, cytokines, cytotoxicity

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