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- Title
Substituted Carbazoles – A New Class of Anthelmintic Agent.
- Authors
Rennison, David; Gueret, Stephanie M.; Laita, Olivia; Bland, Ross J.; Sutherland, Ian A.; Boddy, Ian K.; Brimble, Margaret A.
- Abstract
A series of novel carbazoles were synthesized based on structural modifications to lead carbazole 1 (EC100=2.5 mM against Haemonchus contortus in vitro), which was revealed in a small molecule screening program as a potentially promising platform for the development of new anthelmintic drugs. Subsequently, analogues 19, 21, 41, 42 (EC100=1.25 μM, all), and 39 (EC100=0.625 μM) were demonstrated to exhibit enhanced in vitro anthelmintic activity over the lead structure, with compound 39 also being shown to be active in vivo against Heligmosomoides polygyrus.
- Subjects
CARBAZOLE; CHEMICAL synthesis; ANTHELMINTICS; HAEMONCHUS
- Publication
Australian Journal of Chemistry, 2016, Vol 69, Issue 11, p1268
- ISSN
0004-9425
- Publication type
Article
- DOI
10.1071/CH16169