Journal article icon

Journal article

Structurally simple inhibitors of lanosterol 14alpha-demethylase are efficacious in a rodent model of acute Chagas disease.

Abstract:

We report structure-activity studies of a large number of dialkyl imidazoles as inhibitors of Trypanosoma cruzi lanosterol-14alpha-demethylase (L14DM). The compounds have a simple structure compared to posaconazole, another L14DM inhibitor that is an anti-Chagas drug candidate. Several compounds display potency for killing T. cruzi amastigotes in vitro with values of EC(50) in the 0.4-10 nM range. Two compounds were selected for efficacy studies in a mouse model of acute Chagas disease. At or...

Expand abstract
Publication status:
Published

Actions


Access Document


Publisher copy:
10.1021/jm900030h

Authors


Expand authors...
Journal:
Journal of medicinal chemistry
Volume:
52
Issue:
12
Pages:
3703-3715
Publication date:
2009-06-05
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
URN:
uuid:dd0cf1cb-a068-46a1-954a-8029dd4839b2
Source identifiers:
117669
Local pid:
pubs:117669

Terms of use


Metrics


Views and Downloads






If you are the owner of this record, you can report an update to it here: Report update to this record

TO TOP