Selenophene and thiophene-core estrogen receptor ligands that inhibit motility and development of parasitic stages of Haemonchus contortus

S Preston; J Luo; Y Zhang; A Jabbar; S Crawford; J Baell; A Hofmann; M Hu; HB Zhou; RB Gasser

Journal article

Selenophene and thiophene-core estrogen receptor ligands that inhibit motility and development of parasitic stages of Haemonchus contortus

S Preston, J Luo, Y Zhang, A Jabbar, S Crawford, J Baell, A Hofmann, M Hu, HB Zhou, RB Gasser

Parasites and Vectors | BMC | Published : 2016

DOI: 10.1186/s13071-016-1612-4

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Abstract

Background: Parasitic worms represent a substantial disease burden in animals and humans worldwide. The control of parasitic roundworms (nematodes) relies heavily on the use of anthelmintic drugs. However, widespread drug resistance in nematodes seriously compromises the effectiveness of many anthelmintics around the world. Thus, there is a need to discover new drugs, with unique modes of action, against parasites. Methods: Here, we synthesised and tested 74 selective estrogen receptor modulators (SERMs) for in vitro-activity on parasitic larvae of Haemonchus contortus (barber's pole worm), one of the most important nematode pathogens of small ruminants (including sheep and goats) and a key ..

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University of Melbourne Researchers

Abdul Jabbar Author

Andreas Hofmann Author

Robin B. Gasser Author

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Grants

Awarded by Australian Research Council

Funding Acknowledgements

The present study was funded by the Australian Research Council (ARC), the National Health and Medical Research Council of Australia (NHMRC) and the Wellcome Trust (Pathfinder) (RBG). JB, who is a Larkins Fellow and in receipt of an NHMRC Senior Research Fellowship, also receives funding support from NHMRC and ARC. MH's research is supported by grants from the National Natural Science Foundation of China (NSFC) (no. 31172310), National Key Basic Research Program (973 program) of China (no. 2015CB150300) and the Special Fund for Agro-scientific Research in the Public Interest (no. 201303037). HBZ's research is supported by grants from the NSFC (nos. 81373255, 31371331 and 81573279), Key Scientific Research Project of Ministry of Education of China (313040) and Hubei Province's Outstanding Medical Academic Leader Program. The funding bodies played no role in the design of the study or collection, analysis or interpretation of data, or in the writing of the manuscript.