Farahat, A. A. and Kumar, A. and Wenzler, T. and Brun, R. and Paul, A. and Guo, P. and Wilson, W. D. and Boykin, D. W.. (2023) Investigation of the effect of structure modification of furamidine on the DNA minor groove binding and antiprotozoal activity. Eur J Med Chem, 252. p. 115287.
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Abstract
New analogs of the antiprotozoal agent Furamidine were prepared utilizing Stille coupling reactions and amidation of the bisnitrile intermediate using lithium bis-trimethylsilylamide. Both the phenyl groups and the furan moiety of furamidine were replaced by heterocycles including thiophene, selenophene, indole or benzimidazole. Based upon the DeltaTm and the CD results, the new compounds showed strong binding to the DNA minor groove. The new analogues are also more active both in vitro and in vivo than furamidine. Compounds 7a, 7b, and 7f showed the highest activity in vivo by curing 75% of animals, and this merits further evaluation.
Faculties and Departments: | 09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) 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: | Brun, Reto and Wenzler, Tanja |
Item Type: | Article, refereed |
Article Subtype: | Research Article |
ISSN: | 1768-3254 (Electronic)0223-5234 (Linking) |
Note: | Publication type according to Uni Basel Research Database: Journal article |
Language: | English |
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Last Modified: | 09 May 2023 06:26 |
Deposited On: | 09 May 2023 06:26 |
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