Synthesis, characterization and in vitro antitrypanosomal activities of new carboxamides bearing quinoline moiety.
In: PLoS ONE, Jg. 13 (2018-01-11), Heft 1, S. 1-27
Online
academicJournal
Zugriff:
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 IC 50 range of 1–6 nM (melarsoprol 5 nM). Compound 11n and 11v are more promising antitrypanosomal agents with IC 50 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. [ABSTRACT FROM AUTHOR]
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Synthesis, characterization and in vitro antitrypanosomal activities of new carboxamides bearing quinoline moiety.
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Autor/in / Beteiligte Person: | Ugwu, David Izuchukwu ; Okoro, Uchechukwu Chris ; Mishra, Narendra Kumar |
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Zeitschrift: | PLoS ONE, Jg. 13 (2018-01-11), Heft 1, S. 1-27 |
Veröffentlichung: | 2018 |
Medientyp: | academicJournal |
ISSN: | 1932-6203 (print) |
DOI: | 10.1371/journal.pone.0191234 |
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