Synthesis 1-Acyl-3-(2'-aminophenyl) thioureas as Anti-Intestinal Nematode Prodrugs
Abstract
:1. Introduction
2. Results and Discussion
2.1. Synthesis and Characterization of 1-Acyl-3-(2-aminophenyl) thiourea Derivatives 5a-5h
2.2. Anti-intestinal Nematode Activity
Number of worms recovered from rats (including worms in rats at post mortem) | ||||||
---|---|---|---|---|---|---|
Dose(mg/kg) | 1 | 2 | 3 | Average | Deparasitization(%) | |
Control | 0 | 200 | 198 | 199 | 199 | |
Albendazole | 10 | 0 | 0 | 0 | 0 | 100.00 |
5a | 10 | 180 | 170 | 176 | 175 | 13.7 |
5b | 10 | 178 | 180 | 178 | 178 | 10.5 |
5c | 10 | 183 | 177 | 174 | 178 | 10.5 |
5d | 10 | 188 | 183 | 184 | 185 | 7.0 |
5e | 10 | 177 | 170 | 170 | 172 | 13.5 |
5f | 10 | 109 | 110 | 108 | 109 | 45.2 |
5g | 10 | 108 | 107 | 96 | 103 | 48.2 |
5h | 10 | 22 | 23 | 19 | 21 | 89.4 |
3. Conclusions
4. Experimental
4.1. General
4.2. General Procedure for the Preparation of 1-Acyl-3-(2-aminophenyl)thioureas 5a-5h
4.3. Biological Assays
Acknowledgements
- Sample Availability: Samples of the compounds 5a-5h are available from the authors.
References and Notes
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Duan, L.-P.; Xue, J.; Xu, L.-L.; Zhang, H.-B. Synthesis 1-Acyl-3-(2'-aminophenyl) thioureas as Anti-Intestinal Nematode Prodrugs. Molecules 2010, 15, 6941-6947. https://doi.org/10.3390/molecules15106941
Duan L-P, Xue J, Xu L-L, Zhang H-B. Synthesis 1-Acyl-3-(2'-aminophenyl) thioureas as Anti-Intestinal Nematode Prodrugs. Molecules. 2010; 15(10):6941-6947. https://doi.org/10.3390/molecules15106941
Chicago/Turabian StyleDuan, Li-Ping, Jia Xue, Li-Li Xu, and Hao-Bing Zhang. 2010. "Synthesis 1-Acyl-3-(2'-aminophenyl) thioureas as Anti-Intestinal Nematode Prodrugs" Molecules 15, no. 10: 6941-6947. https://doi.org/10.3390/molecules15106941