Design, Synthesis and Biological Evaluation of New Imidazo[2,1-b]Thiazole Derivatives as Selective COX-2 Inhibitors
| Author | Mahsa Shahrasbi | en |
| Author | Mahsa Azami Movahed | en |
| Author | Orkideh Ghorban Dadras | en |
| Author | Bahram Daraei | en |
| Author | Afshin Zarghi | en |
| Issued Date | 2018-10-31 | en |
| Abstract | A new series of imidazo[2,1-b]thiazole analogs containing a methyl sulfonyl COX-2 pharmacophore was synthesized and evaluated for their COX-2 inhibitory activity. According to in-vitro COX-1/COX-2 inhibition data, all compounds (6a-g) were selective inhibitors of COX-2 isoenzyme with IC50 values in the highly potent 0.08-0.16 µM range. These results indicated that both potency and selectivity of COX-2 inhibitory activity were affected by the type and size of amine on C-5 of imidazo[2,1-b]thiazole ring. Our data identified N,N-dimethyl-1-(6-(4-(methylsulfonyl)phenyl)imidazo[2,1-b]thiazol-5-yl)methanamine (6a) as a potent and selective COX-2 inhibitor (IC50 COX-1 >100 µM; IC50 COX-2 = 0.08 µM; selectivity index = 313.7). Our results indicated that both potency and selectivity of COX-2 inhibitory activity were affected by the type and size of amine on C-5 of imidazo[2,1-b]thiazole ring. | en |
| DOI | https://doi.org/10.22037/ijpr.2018.2304 | en |
| Keyword | Design | en |
| Keyword | Synthesis | en |
| Keyword | Cyclooxygenase-2 inhibition | en |
| Keyword | Imidazo[2 | en |
| Keyword | 1-b]Thiazole | en |
| Keyword | Molecular modeling | en |
| Publisher | Brieflands | en |
| Title | Design, Synthesis and Biological Evaluation of New Imidazo[2,1-b]Thiazole Derivatives as Selective COX-2 Inhibitors | en |
| Type | Original Article | en |
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