1-Methyl-1H-pyrazole-5-carboxamide Derivatives Exhibit Unexpected Acute Mammalian Toxicity

Autor: Nghi H. Nguyen, Abdul Jabbar, Fei Huang, Sean L. McGee, Yaqing Jiao, Abhijit Kundu, Michael J. Palmer, Banfeng Ruan, Bill C.H. Chang, Thuy G. Le, Jonathan B. Baell, Liam G. Hall, Atanu Ghoshal, Lian Xue, Jose F. Garcia-Bustos, Robin B. Gasser, Timothy N. C. Wells, Sarah Preston, Sheree D. Martin

Publikováno v: Journal of Medicinal Chemistry. 64:840-844

A series of 1-methyl-1H-pyrazole-5-carboxamides were synthesized as potent inhibitors of the parasitic nematode of sheep, Haemonchus contortus. These compounds did not show overt cytotoxicity to a range of mammalian cell lines under standard in vitro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8c0ce81985631a42c44c923ffeabc447
https://doi.org/10.1021/acs.jmedchem.0c01793

Structure–Activity Relationship Studies of Tolfenpyrad Reveal Subnanomolar Inhibitors of Haemonchus contortus Development

Autor: Thuy G. Le, Nghi H. Nguyen, Jose F. Garcia-Bustos, Yaqing Jiao, Andreas Hofmann, Banfeng Ruan, Abdul Jabbar, Abhijit Kundu, Robin B. Gasser, Jonathan B. Baell, Sarah Preston, Timothy N. C. Wells, Bill C.H. Chang, Atanu Ghoshal, Fei Huang, Michael J. Palmer, Jennifer Keiser, Lian Xue

Publikováno v: Journal of Medicinal Chemistry. 62:1036-1053

Recently, we have discovered that the registered pesticide, tolfenpyrad, unexpectedly and potently inhibits the development of the L4 larval stage of the parasitic nematode Haemonchus contortus with an IC50 value of 0.03 μM while displaying good sel

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::47491ab1c7d20250ab7a12c0a1392ab5
https://doi.org/10.1021/acs.jmedchem.8b01789

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

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

Publikováno v: European journal of medicinal chemistry. 190

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 d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d4429c32c56200b5ad074909d665987e
https://pubmed.ncbi.nlm.nih.gov/32018095

Tetrahydroquinoxalines induce a lethal evisceration phenotype in Haemonchus contortus in vitro

Autor: Yaqing Jiao, Jill Danne, Sabatino Ventura, Jose F. Garcia-Bustos, Tao Wang, Bill C.H. Chang, Cameron Skinner, Thuy G. Le, Nghi H. Nguyen, Jonathan B. Baell, Antony Botteon, Nicole McNamara, Anson V. Koehler, Andreas Hofmann, Sarah Preston, Robin B. Gasser, Sarah Ellis, Abdul Jabbar

Publikováno v: International Journal for Parasitology: Drugs and Drug Resistance
International Journal for Parasitology: Drugs and Drug Resistance, Vol 9, Iss, Pp 59-71 (2019)

In the present study, the anthelmintic activity of a human tyrosine kinase inhibitor, AG-1295, and 14 related tetrahydroquinoxaline analogues against Haemonchus contortus was explored. These compounds were screened against parasitic larvae - exsheath

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::594b500dbc656e32122027a49de92f90
https://pubmed.ncbi.nlm.nih.gov/30690282