New Amides of 5-(4-Chlorobenzoyl)aminoorotic Acid: Their Synthesis and Biological Activity
| Autor: | Magdalena Śpiewak, Ryszard Jasztold-Howorko, Ryszard Międzybrodzki, Andrzej Regiec |
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| Rok vydání: | 2008 |
| Předmět: |
Orotic Acid
Isothiazole Molecular Structure Pyrimidine Stereochemistry Anti-Inflammatory Agents Pharmaceutical Science Biological activity Lymphocyte Activation Nitric Oxide Ring (chemistry) Amides Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound chemistry Amide Biological property Drug Discovery Cytokines Humans Lymphocytes Immunosuppressive Agents Biological evaluation |
| Zdroj: | Archiv der Pharmazie. 341:677-689 |
| ISSN: | 1521-4184 0365-6233 |
| DOI: | 10.1002/ardp.200800034 |
| Popis: | The synthesis and in-vitro biological evaluation of the amide series 4 of 5-(4-chlorobenzoyl)aminoorotic acid 2 are presented. The biological properties of a few 5-(4-chlorobenzoyl)amino-2,6-dihydroxy-N-substituted-4-pyrimidinecarboxamide derivatives 4 tested here were compared with those of the isosteric isothiazole derivative MR-2/94 (5-(4-chlorobenzoyl)amino-N-(4-chlorophenyl)-3-methyl-4-isothiazolecarboxamide), which possesses a strong immunosuppressive and anti-inflammatory activity [1, 2], It must be suggested that replacement of the isothiazole by a pyrimidine core ring system resulted in considerable lowering of the anti-inflammatory and immunotropic actions of the obtained amides. Physicochemical properties of 2-(4-chlorophenyl)-6,8-dihydroxy-4H-pyrimido[5,4-d]-1,3-oxazin-4-on 3 are also briefly described. |
| Databáze: | OpenAIRE |
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