Academic Journal
Antimalarial N1,N3-dialkyldioxonaphthoimidazoliums: synthesis, biological activity, and structure-activity relationships
| العنوان: | Antimalarial N1,N3-dialkyldioxonaphthoimidazoliums: synthesis, biological activity, and structure-activity relationships |
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| المؤلفون: | Ahenkorah, S., Coertzen, D., Tong, J. X., Fridianto, K., Wittlin, S., Birkholtz, L. M., Tan, K. S. W., Lam, Y., Go, M. L., Haynes, R. K. |
| بيانات النشر: | American Chemical Society |
| سنة النشر: | 2020 |
| المجموعة: | University of Basel: edoc |
| الوصف: | Here we report the nanomolar potencies of N (1),N (3)-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 N(1)/N(3) alkyl residues on the scaffold. Gametocytocidal activity was also detected, with most members active at IC50 < 1 muM. A representative analog with good solubility, limited PAMPA permeability, and microsomal stability demonstrated oral efficacy on a humanized mouse model of P. falciparum. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | unknown |
| تدمد: | 1948-5875 |
| Relation: | Ahenkorah, S. and Coertzen, D. and Tong, J. X. and Fridianto, K. and Wittlin, S. and Birkholtz, L. M. and Tan, K. S. W. and Lam, Y. and Go, M. L. and Haynes, R. K. (2020) Antimalarial N1,N3-dialkyldioxonaphthoimidazoliums: synthesis, biological activity, and structure-activity relationships. ACS medicinal chemistry letters, 11. pp. 49-55.; info:pmid/31938463; urn:ISSN:1948-5875 |
| DOI: | 10.1021/acsmedchemlett.9b00457 |
| الاتاحة: | https://edoc.unibas.ch/75569/ https://doi.org/10.1021/acsmedchemlett.9b00457 |
| Rights: | info:eu-repo/semantics/closedAccess |
| رقم الانضمام: | edsbas.B8E204C1 |
| قاعدة البيانات: | BASE |
Full Text Finder | تدمد: | 19485875 |
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| DOI: | 10.1021/acsmedchemlett.9b00457 |