Synthesis and Evaluation of Chalcone-Quinoline Based Molecular Hybrids as Potential Anti-Malarial Agents
| dc.contributor.author | Vinindwa, Bonani | |
| dc.contributor.author | Dziwornu, Godwin Akpeko | |
| dc.contributor.author | Masamba, Wayiza | |
| dc.date.accessioned | 2021-10-11T09:47:53Z | |
| dc.date.available | 2021-10-11T09:47:53Z | |
| dc.date.issued | 2021-07-05 | |
| dc.date.updated | 2021-07-08T14:23:40Z | |
| dc.description.abstract | Molecular hybridization is a drug discovery strategy that involves the rational design of new chemical entities by the fusion (usually via a covalent linker) of two or more drugs, both active compounds and/or pharmacophoric units recognized and derived from known bioactive molecules. The expected outcome of this chemical modification is to produce a new hybrid compound with improved affinity and efficacy compared to the parent drugs. Additionally, this strategy can result in compounds presenting modified selectivity profiles, different and/or dual modes of action, reduced undesired side effects and ultimately lead to new therapies. In this study, molecular hybridization was used to generate new molecular hybrids which were tested against the chloroquine sensitive (NF54) strain of <i>P. falciparum</i>. To prepare the new molecular hybrids, the quinoline nucleus, one of the privileged scaffolds, was coupled with various chalcone derivatives via an appropriate linker to produce a total of twenty-two molecular hybrids in 11%–96% yield. The synthesized compounds displayed good antiplasmodial activity with IC<sub>50</sub> values ranging at 0.10–4.45 μM. | |
| dc.identifier | doi: 10.3390/molecules26134093 | |
| dc.identifier.apacitation | Vinindwa, B., Dziwornu, G. A., & Masamba, W. (2021). Synthesis and Evaluation of Chalcone-Quinoline Based Molecular Hybrids as Potential Anti-Malarial Agents. http://hdl.handle.net/11427/35156 | en_ZA |
| dc.identifier.chicagocitation | Vinindwa, Bonani, Godwin Akpeko Dziwornu, and Wayiza Masamba "Synthesis and Evaluation of Chalcone-Quinoline Based Molecular Hybrids as Potential Anti-Malarial Agents." (2021) http://hdl.handle.net/11427/35156 | en_ZA |
| dc.identifier.citation | Vinindwa, B., Dziwornu, G.A. & Masamba, W. 2021. Synthesis and Evaluation of Chalcone-Quinoline Based Molecular Hybrids as Potential Anti-Malarial Agents. http://hdl.handle.net/11427/35156 | en_ZA |
| dc.identifier.ris | TY - Journal Article AU - Vinindwa, Bonani AU - Dziwornu, Godwin Akpeko AU - Masamba, Wayiza AB - Molecular hybridization is a drug discovery strategy that involves the rational design of new chemical entities by the fusion (usually via a covalent linker) of two or more drugs, both active compounds and/or pharmacophoric units recognized and derived from known bioactive molecules. The expected outcome of this chemical modification is to produce a new hybrid compound with improved affinity and efficacy compared to the parent drugs. Additionally, this strategy can result in compounds presenting modified selectivity profiles, different and/or dual modes of action, reduced undesired side effects and ultimately lead to new therapies. In this study, molecular hybridization was used to generate new molecular hybrids which were tested against the chloroquine sensitive (NF54) strain of <i>P. falciparum</i>. To prepare the new molecular hybrids, the quinoline nucleus, one of the privileged scaffolds, was coupled with various chalcone derivatives via an appropriate linker to produce a total of twenty-two molecular hybrids in 11%–96% yield. The synthesized compounds displayed good antiplasmodial activity with IC<sub>50</sub> values ranging at 0.10–4.45 μM. DA - 2021-07-05 DB - OpenUCT DP - University of Cape Town LK - https://open.uct.ac.za PY - 2021 T1 - Synthesis and Evaluation of Chalcone-Quinoline Based Molecular Hybrids as Potential Anti-Malarial Agents TI - Synthesis and Evaluation of Chalcone-Quinoline Based Molecular Hybrids as Potential Anti-Malarial Agents UR - http://hdl.handle.net/11427/35156 ER - | en_ZA |
| dc.identifier.uri | http://hdl.handle.net/11427/35156 | |
| dc.identifier.vancouvercitation | Vinindwa B, Dziwornu GA, Masamba W. Synthesis and Evaluation of Chalcone-Quinoline Based Molecular Hybrids as Potential Anti-Malarial Agents. 2021; http://hdl.handle.net/11427/35156. | en_ZA |
| dc.publisher | Multidisciplinary Digital Publishing Institute | |
| dc.source.uri | https://www.mdpi.com/journal/molecules | |
| dc.title | Synthesis and Evaluation of Chalcone-Quinoline Based Molecular Hybrids as Potential Anti-Malarial Agents | |
| dc.type | Journal Article |