- Title
- Arylpyrrole and fipronil analogues that inhibit the motility and/or development of Haemonchus contortus in vitro
- Creator
- Herath, Dilrukshi; Song, Hongjian; Preston, Sarah; Jabbar, Abdul; Wang, Tao; McGee, Sean; Hofmann, Andreas; Garcia-Bustos, Jose; Chang, Bill; Koehler, Anson; Liu, Yuxiu; Ma, Qiaoqiao; Zhang, Penqxiang; Zhao, Qiqi; Wang, Qingmin; Gasser, Robin
- Date
- 2018
- Type
- Text; Journal article
- Identifier
- http://researchonline.federation.edu.au/vital/access/HandleResolver/1959.17/167730
- Identifier
- vital:13687
- Identifier
-
https://doi.org/10.1016/j.ijpddr.2018.06.002
- Identifier
- ISBN:2211-3207
- Abstract
- Due to widespread drug resistance in parasitic nematodes, there is a need to develop new anthelmintics. Given the cost and time involved in developing a new drug, the repurposing of known chemicals can be a promising, alternative approach. In this context, we tested a library (n = 600) of natural product-inspired pesticide analogues against exsheathed third stage-larvae (xL3s) of Haemonchus contortus (barber's pole worm) using a whole-organism, phenotypic screening technique that measures the inhibition of motility and development in treated larvae. In the primary screen, we identified 32 active analogues derived from chemical scaffolds of arylpyrrole or fipronil. The seven most promising compounds, selected based on their anthelmintic activity and/or limited cytotoxicity, are arylpyrroles that reduced the motility of fourth-stage larvae (L4s) with significant potency (IC 50 values ranged from 0.04 ± 0.01
- Publisher
- Elsevier Ltd
- Relation
- International Journal for Parasitology: Drugs and Drug Resistance Vol. 8, no. 3 (2018), p. 379-385
- Rights
- http://creativecommons.org/licenses/BY-NC-ND/4.0/
- Rights
- Copyright © 2018 The Authors. Published by Elsevier Ltd on behalf of Australian Society for Parasitology. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/BY-NC-ND/4.0/).
- Rights
- Open Access
- Rights
- This metadata is freely available under a CCO license
- Subject
- 1108 Medical Microbiology; Arylpyrrole; Fipronil; Haemonchus contortus; Anthelmintic; Drug discovery
- Full Text
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