List of Titles

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

- Preston, Sarah, Luo, Junjie, Zhang, Yuezhou, Jabbar, Abdul, Crawford, Simon, Baell, Jonathan, Hofmann, Andreas, Hu, Min, Zhou, Hai-Bing, Gasser, Robin

Authors: Preston, Sarah , Luo, Junjie , Zhang, Yuezhou , Jabbar, Abdul , Crawford, Simon , Baell, Jonathan , Hofmann, Andreas , Hu, Min , Zhou, Hai-Bing , Gasser, Robin
Date: 2016
Type: Text , Journal article
Relation: Parasites & Vectors Vol. 9, no. 1 (2016), p. 346
Full Text: false
Reviewed:
Description: 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.

Synthesis and structure-activity relationship study of pyrrolidine-oxadiazoles as anthelmintics against Haemonchus contortus

- Ruan, Banfeng, Zhang, Yuezhou, Tadesse, Solomon, Preston, Sarah, Taki, Aya, Jabbar, Abdul, Hofmann, Andreas, Jiao, Yaqing, Garcia-Bustos, Jose, Harjani, Jitendra, Le, Thuy, Varghese, Swapna, Teguh, Silvia, Xie, Yiyue, Odiba, Jephthah, Hu, Min, Gasser, Robin, Baell, Jonathan

Authors: Ruan, Banfeng , Zhang, Yuezhou , Tadesse, Solomon , Preston, Sarah , Taki, Aya , Jabbar, Abdul , Hofmann, Andreas , Jiao, Yaqing , Garcia-Bustos, Jose , Harjani, Jitendra , Le, Thuy , Varghese, Swapna , Teguh, Silvia , Xie, Yiyue , Odiba, Jephthah , Hu, Min , Gasser, Robin , Baell, Jonathan
Date: 2020
Type: Text , Journal article
Relation: European Journal of Medicinal Chemistry Vol. 190, no. (2020), p.
Full Text: false
Reviewed:
Description: Parasitic roundworms (nematodes) are significant pathogens of humans and animals and cause substantive socioeconomic losses due to the diseases that they cause. The control of nematodes in livestock animals relies heavily on the use of anthelmintic drugs. However, their extensive use has led to a widespread problem of drug resistance in these worms. Thus, the discovery and development of novel chemical entities for the treatment of parasitic worms of humans and animals is needed. Herein, we describe our medicinal chemistry optimization efforts of a phenotypic hit against Haemonchus contortus based on a pyrrolidine-oxadiazole scaffold. This led to the identification of compounds with potent inhibitory activities (IC50 = 0.78–22.4 μM) on the motility and development of parasitic stages of H. contortus, and which were found to be highly selective in a mammalian cell counter-screen. These compounds could be used as suitable chemical tools for drug target identification or as lead compounds for further optimization. © 2020 Elsevier Masson SAS

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