Synthesis, Characterization and Biological Activity of Some Dithiourea Derivatives
| Autor: | Felix Odame, Eric Hosten, Jason Krause, Michelle Isaacs, Heinrich Hoppe, Setshaba D Khanye, Yasien Sayed, Carminita Frost, Kevin Lobb, Zenixole Tshentu |
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| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: | |
| Zdroj: | Acta Chimica Slovenica, Vol 67, Iss 3, Pp 764-777 (2020) |
| Druh dokumentu: | article |
| ISSN: | 1318-0207 1580-3155 |
| DOI: | 10.17344/acsi.2019.5689 |
| Popis: | Novel dithiourea derivatives have been designed as HIV-1 protease inhibitors using Autodock 4.2, synthesized and characterized by spectroscopic methods and microanalysis. 1-(3-Bromobenzoyl)-3-[2-({[(3-bromophenyl)formamido]methanethioyl}amino)phenyl]thiourea (10) and 3-benzoyl-1{[(phenylformamido)methanethioyl]amino}thiourea (12) gave a percentage viability of 17.9±5.6% and 11.2±0.9% against Trypanosoma brucei. Single crystal X-ray diffraction analysis of 1-benzoyl-3-(5-methyl-2-{[(phenylformamido)methanethioyl]amino}phenyl)thiourea (1), 3-benzoyl-1-(2-{[(phenylformamido)methanethioyl]amino}ethyl)thiourea (11), 3-benzoyl-1-{[(phenylformamido)methanethioyl]amino}thiourea (12) and 3-benzoyl-1-(4-{[(phenylformamido)methanethioyl]amino}butyl)thiourea (14) have been presented. 1-(3-Bromobenzoyl)-3-[2-({[(3-bromophenyl)formamido]methanethioyl}amino)phenyl]thiourea (10) gave a percentage inhibition of 97.03±0.37% against HIV-1 protease enzyme at a concentration of 100 µM. |
| Databáze: | Directory of Open Access Journals |
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