Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UMLS:C0024530 (
malaria
)
44,886
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Malaria
remains one of the most deadly infectious diseases, causing hundreds of thousands of deaths each year, primarily in young children and pregnant mothers. Here, we report the discovery and derivatization of a series of pyrazolo[3,4-
b
]pyridines targeting
Plasmodium falciparum
, the deadliest species of the
malaria
parasite. Hit compounds in this series display sub-micromolar
in vitro
activity against the intraerythrocytic stage of the parasite as well as little to no toxicity against the human fibroblast BJ and liver HepG2 cell lines. In addition, our hit compounds show good activity against the liver stage of the parasite but little activity against the gametocyte stage. Parasitological profiles, including rate of killing, docking, and molecular dynamics studies, suggest that our compounds may target the Q
o
binding site of
cytochrome
bc
1
.
...
PMID:Synthesis and Structure-Activity Relationship of Dual-Stage Antimalarial Pyrazolo[3,4-
b
]pyridines. 3294 66
<< Previous
1
2
3
4
5
6
7
8
9
