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Substituted carbazoles: a new class of anthelmintic agent

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journal contribution
posted on 2023-05-03, 15:03 authored by D. Rennison, S.M. Gueret, O. Laita, Ross Bland, Ian SutherlandIan Sutherland, I.K. Boddy, M.A. Brimble
A series of novel carbazoles were synthesized based on structural modifications to lead carbazole 1 (EC100≤2.5M 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≤ 1.25M, all), and 39 (EC100≤0.625M) 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.

History

Rights statement

© CSIRO 1996-2017

Language

  • English

Does this contain Māori information or data?

  • No

Publisher

CSIRO Publishing

Journal title

Australian Journal of Chemistry

ISSN

0004-9425

Citation

Rennison, D., Gueret, S. M., Laita, O., Bland, R. J., Sutherland, I. A., Boddy, I. K., & Brimble, M. A. (2016). Substituted carbazoles: a new class of anthelmintic agent. Australian Journal of Chemistry, 69(11), 1268–1276. doi:10.1071/CH16169