Attram, H. D. and Wittlin, S. and Chibale, K.. (2019) Incorporation of an intramolecular hydrogen bonding motif in the side chain of antimalarial benzimidazoles. MedChemComm , 10 (3). pp. 450-455.
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Official URL: https://edoc.unibas.ch/70114/
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Abstract
Analogues of a novel class of benzimidazoles with an intramolecular hydrogen bonding motif have been synthesized and evaluated in vitro for their antiplasmodium activity against chloroquine-sensitive (NF54) and multi-drug resistant (K1) strains of the human malaria parasite Plasmodium falciparum. Compounds were also screened for their cytotoxicity towards a mammalian Chinese hamster ovarian (CHO) cell line. Most of the compounds exhibited good antiplasmodium activity (PfNF54 IC50 <1 μM) and were relatively noncytotoxic. Moreover, towards establishing the possible mode of action of these molecules, inhibition of beta-hematin formation was investigated and two compounds were found to be inhibitors. Single crystal X-ray data confirmed the existence of an intramolecular hydrogen bond.
Faculties and Departments: | 09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser) |
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UniBasel Contributors: | Wittlin, Sergio |
Item Type: | Article, refereed |
Article Subtype: | Research Article |
Publisher: | Royal Society of Chemistry |
ISSN: | 2040-2503 |
e-ISSN: | 2040-2511 |
Note: | Publication type according to Uni Basel Research Database: Journal article |
Identification Number: |
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Last Modified: | 04 Apr 2019 12:02 |
Deposited On: | 04 Apr 2019 12:02 |
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