Synthesis of a Novel Siliconized Analog of Clofibrate (Silafibrate) and Comparison of their Anti-inflammatory Activities
| Author | Mojtaba Ziaee | en |
| Author | Morteza Samini | en |
| Author | Mohammad Bolourtchian | en |
| Author | Mohammad Ghaffarzadeh | en |
| Author | Maryam Ahmadi | en |
| Author | Mohammad Ali Egbal | en |
| Author | Arash Khorrami | en |
| Author | Sina Andalib | en |
| Author | Nasrin Maleki-Dizaji | en |
| Author | Alireza Garjani | en |
| Issued Date | 2012-01-31 | en |
| Abstract | Fibrates, as hypolipidemic drugs known as agonists of peroxisome proliferator-activated receptors, diminish inflammatory responses. Studies have shown that incorporation of a silicon atom into a drug structure improves its pharmacological potency, modifies its selectivity toward a given target, or changes its metabolic rate, in addition to increasing the lipophilicity of the compounds. A siliconized analog of clofibrate, ethyl-2-methyl-2-(4-(trimethylsilyl)phenoxy)propionate was synthesized, whereby the chlorine atom in the phenoxy ring was replaced by a trimethylsilyl group. The anti-inflammatory effects of the siliconized analog (silafibrate) were evaluated in an air-pouch model of inflammation and compared with those of clofibrate. Oral administration of both drugs produced a significant anti-inflammatory action by reducing carrageenan induced pouch leukocyte recruitment, exudates production, and granulated tissue weight. The silicon isostere of clofibrate has improved anti-inflammatory properties. | en |
| DOI | https://doi.org/10.22037/ijpr.2011.1045 | en |
| URI | https://brieflands.com/journals/ijpr/articles/125767 | en |
| Keyword | Clofibrate | en |
| Keyword | Silicon | en |
| Keyword | Siliconized analog | en |
| Keyword | Anti-inflammatory | en |
| Publisher | Brieflands | en |
| Title | Synthesis of a Novel Siliconized Analog of Clofibrate (Silafibrate) and Comparison of their Anti-inflammatory Activities | en |
| Type | Original Article | en |
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