期刊
MEDICINAL CHEMISTRY RESEARCH
卷 27, 期 8, 页码 1876-1884出版社
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-018-2199-4
关键词
Malaria; Plasmodium falciparum; Pyrazolopyrimidine; Sulfonamide
资金
- Coordination of Improvement of Higher Education (CAPES)
- National Council of R&D of Brazil (CNPq)
- Foundation for Research of the State of Rio de Janeiro (FAPERJ)
- Technological Development Program on Products for Health (PDTIS)
- CNPq
- FAPERJ
Nine 1-phenyl-1H-pyrazolo[3,4-d]pyrimidine derivatives with different substituents in the 4-position of the phenyl group and benzenesulfonamide moiety were synthesized and evaluated against Plasmodium falciparum. Six compounds exhibited activity in vitro against the chloroquine-resistant clone W2 with IC50 values ranging from 5.13 to 12.22 A mu M. The most active derivative with substituents R-1 = F / R-2 = CH3 exhibited an IC50 value of 5.13 A mu M and an IS value of 62.90, which was higher than that of the control drug sulfadoxine. For this reason, it is possible to conclude that the 1H-pyrazolo[3,4-d]pyrimidine system is promising as a prototype for further studies of antimalarial candidates.
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