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- Title
A New Synthetic Route to Original Sulfonamide Derivatives in 2-Trichloromethylquinazoline Series: A Structure-Activity Relationship Study of Antiplasmodial Activity.
- Authors
Primas, Nicolas; Verhaeghe, Pierre; Cohen, Anita; Kieffer, Charline; Dumètre, Aurélien; Hutter, Sébastien; Rault, Sylvain; Rathelot, Pascal; Azas, Nadine; Vanelle, Patrice
- Abstract
We report herein a simple and efficient two-step synthetic approach to new 2-trichloromethylquinazolines possessing a variously substituted sulfonamide group at position 4 used to prepare new quinazolines with antiparasitic properties. Thus, an original series of 20 derivatives was synthesized, which proved to be less-toxic than previously synthesized hits on the human HepG2 cell line, but did not display significant antiplasmodial activity. A brief Structure-Activity Relationship (SAR) evaluation shows that a more restricted conformational freedom is probably necessary for providing antiplasmodial activity.
- Subjects
SULFONAMIDES; STRUCTURE-activity relationships; QUINAZOLINE; ANTIPARASITIC agents; CELL lines; TRICHLOROMETHYL group
- Publication
Molecules, 2012, Vol 17, Issue 7, p8105
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules17078105