Please use this identifier to cite or link to this item:
https://doi.org/10.1021/acsmedchemlett.9b00457
DC Field | Value | |
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dc.title | Antimalarial N-1,N-3-Dialkyldioxonaphthoimidazoliums: Synthesis, Biological Activity, and Structure-activity Relationships | |
dc.contributor.author | Ahenkorah, Stephen | |
dc.contributor.author | Coertzen, Dina | |
dc.contributor.author | Tong, Jie Xin | |
dc.contributor.author | Fridianto, Kevin | |
dc.contributor.author | Wittlin, Sergio | |
dc.contributor.author | Birkholtz, Lyn-Marie | |
dc.contributor.author | Tan, Kevin SW | |
dc.contributor.author | Lam, Yulin | |
dc.contributor.author | Go, Mei-Lin | |
dc.contributor.author | Haynes, Richard K | |
dc.date.accessioned | 2023-07-10T08:54:39Z | |
dc.date.available | 2023-07-10T08:54:39Z | |
dc.date.issued | 2020-01-09 | |
dc.identifier.citation | Ahenkorah, Stephen, Coertzen, Dina, Tong, Jie Xin, Fridianto, Kevin, Wittlin, Sergio, Birkholtz, Lyn-Marie, Tan, Kevin SW, Lam, Yulin, Go, Mei-Lin, Haynes, Richard K (2020-01-09). Antimalarial N-1,N-3-Dialkyldioxonaphthoimidazoliums: Synthesis, Biological Activity, and Structure-activity Relationships. ACS MEDICINAL CHEMISTRY LETTERS 11 (1) : 49-55. ScholarBank@NUS Repository. https://doi.org/10.1021/acsmedchemlett.9b00457 | |
dc.identifier.issn | 1948-5875 | |
dc.identifier.uri | https://scholarbank.nus.edu.sg/handle/10635/242992 | |
dc.description.abstract | Here we report the nanomolar potencies of N1,N3-dialkyldioxonaphthoimidazoliums against asexual forms of sensitive and resistant Plasmodium falciparum. Activity was dependent on the presence of the fused quinone-imidazolium entity and lipophilicity imparted by the N1/N3 alkyl residues on the scaffold. Gametocytocidal activity was also detected, with most members active at IC50 < 1 μM. A representative analog with good solubility, limited PAMPA permeability, and microsomal stability demonstrated oral efficacy on a humanized mouse model of P. falciparum. | |
dc.language.iso | en | |
dc.publisher | AMER CHEMICAL SOC | |
dc.source | Elements | |
dc.subject | Science & Technology | |
dc.subject | Life Sciences & Biomedicine | |
dc.subject | Chemistry, Medicinal | |
dc.subject | Pharmacology & Pharmacy | |
dc.subject | Antimalarials | |
dc.subject | dioxonaphthoimidazoliums | |
dc.subject | quinones | |
dc.subject | drug resistant asexual parasites | |
dc.subject | gametocytocidal activity | |
dc.subject | DRUG | |
dc.subject | COMPOUND | |
dc.subject | MALARIA | |
dc.subject | ASSAY | |
dc.subject | YM155 | |
dc.type | Article | |
dc.date.updated | 2023-07-10T08:05:04Z | |
dc.contributor.department | CHEMISTRY | |
dc.contributor.department | MICROBIOLOGY AND IMMUNOLOGY | |
dc.contributor.department | PHARMACY | |
dc.contributor.department | DUKE-NUS MEDICAL SCHOOL | |
dc.description.doi | 10.1021/acsmedchemlett.9b00457 | |
dc.description.sourcetitle | ACS MEDICINAL CHEMISTRY LETTERS | |
dc.description.volume | 11 | |
dc.description.issue | 1 | |
dc.description.page | 49-55 | |
dc.published.state | Published | |
Appears in Collections: | Staff Publications Elements |
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