Synthesis, characterization and in vitro antitrypanosomal activities of new carboxamides bearing quinoline moiety.
The reported toxicities of current antitrypanosomal drugs and the emergence of drug resistant trypanosomes underscore the need for the development of new antitrypanosomal agents. We report herein the synthesis and antitrypanosomal activity of 24 new amide derivatives of 3-aminoquinoline, bearing sub...
| Main Authors: | , , |
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| Format: | Article |
| Language: | English |
| Published: |
Public Library of Science (PLoS)
2018-01-01
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| Series: | PLoS ONE |
| Online Access: | http://europepmc.org/articles/PMC5764481?pdf=render |
| _version_ | 1818557660068315136 |
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| author | David Izuchukwu Ugwu Uchechukwu Chris Okoro Narendra Kumar Mishra |
| author_facet | David Izuchukwu Ugwu Uchechukwu Chris Okoro Narendra Kumar Mishra |
| author_sort | David Izuchukwu Ugwu |
| collection | DOAJ |
| description | The reported toxicities of current antitrypanosomal drugs and the emergence of drug resistant trypanosomes underscore the need for the development of new antitrypanosomal agents. We report herein the synthesis and antitrypanosomal activity of 24 new amide derivatives of 3-aminoquinoline, bearing substituted benzenesulphonamide. Nine of the new derivatives showed comparable antitrypanosomal activities at IC50 range of 1-6 nM (melarsoprol 5 nM). Compound 11n and 11v are more promising antitrypanosomal agents with IC50 1.0 nM than the rest of the reported derivatives. The novel compounds showed satisfactory predicted physico-chemical properties including oral bioavailability, permeability and transport properties. |
| first_indexed | 2024-12-14T00:02:31Z |
| format | Article |
| id | doaj.art-0088e4c989c043b696732c8926e70eae |
| institution | Directory Open Access Journal |
| issn | 1932-6203 |
| language | English |
| last_indexed | 2024-12-14T00:02:31Z |
| publishDate | 2018-01-01 |
| publisher | Public Library of Science (PLoS) |
| record_format | Article |
| series | PLoS ONE |
| spelling | doaj.art-0088e4c989c043b696732c8926e70eae2022-12-21T23:26:14ZengPublic Library of Science (PLoS)PLoS ONE1932-62032018-01-01131e019123410.1371/journal.pone.0191234Synthesis, characterization and in vitro antitrypanosomal activities of new carboxamides bearing quinoline moiety.David Izuchukwu UgwuUchechukwu Chris OkoroNarendra Kumar MishraThe reported toxicities of current antitrypanosomal drugs and the emergence of drug resistant trypanosomes underscore the need for the development of new antitrypanosomal agents. We report herein the synthesis and antitrypanosomal activity of 24 new amide derivatives of 3-aminoquinoline, bearing substituted benzenesulphonamide. Nine of the new derivatives showed comparable antitrypanosomal activities at IC50 range of 1-6 nM (melarsoprol 5 nM). Compound 11n and 11v are more promising antitrypanosomal agents with IC50 1.0 nM than the rest of the reported derivatives. The novel compounds showed satisfactory predicted physico-chemical properties including oral bioavailability, permeability and transport properties.http://europepmc.org/articles/PMC5764481?pdf=render |
| spellingShingle | David Izuchukwu Ugwu Uchechukwu Chris Okoro Narendra Kumar Mishra Synthesis, characterization and in vitro antitrypanosomal activities of new carboxamides bearing quinoline moiety. PLoS ONE |
| title | Synthesis, characterization and in vitro antitrypanosomal activities of new carboxamides bearing quinoline moiety. |
| title_full | Synthesis, characterization and in vitro antitrypanosomal activities of new carboxamides bearing quinoline moiety. |
| title_fullStr | Synthesis, characterization and in vitro antitrypanosomal activities of new carboxamides bearing quinoline moiety. |
| title_full_unstemmed | Synthesis, characterization and in vitro antitrypanosomal activities of new carboxamides bearing quinoline moiety. |
| title_short | Synthesis, characterization and in vitro antitrypanosomal activities of new carboxamides bearing quinoline moiety. |
| title_sort | synthesis characterization and in vitro antitrypanosomal activities of new carboxamides bearing quinoline moiety |
| url | http://europepmc.org/articles/PMC5764481?pdf=render |
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