Jose Garcia-Bustos

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

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

Journal article  |  2021  |  JOURNAL OF MEDICINAL CHEMISTRY

A series of 1-methyl-1H-pyrazole-5-carboxamides were synthesized as potent inhibitors of the parasitic nematode of sheep, Haemonch..

Human Aurora kinase inhibitor Hesperadin reveals epistatic interaction between Plasmodium falciparum PfArk1 and PfNek1 kinases.

Belinda J Morahan, Clarissa Abrie, Keith Al-Hasani, Mitchell B Batty, Victoria Corey, Anne N Cowell, Jandeli Niemand, Elizabeth A Winzeler, Lyn-Marie Birkholtz, Christian Doerig, Jose F Garcia-Bustos

Journal article  |  2020  |  Commun Biol

Mitosis has been validated by numerous anti-cancer drugs as being a druggable process, and selective inhibition of parasite prolif..

Interaction of Plasmodium falciparum casein kinase 1 with components of host cell protein trafficking machinery

Mitchell B Batty, Ralf B Schittenhelm, Dominique Dorin-Semblat, Christian Doerig, Jose F Garcia-Bustos

Journal article  |  2020  |  IUBMB LIFE

A pool of Plasmodium falciparum casein kinase 1 (PfCK1) has been shown to localize to the host red blood cell (RBC) membrane and b..

Synthetic Kavalactone Analogues with Increased Potency and Selective Anthelmintic Activity against Larvae of Haemonchus contortus In Vitro

HMP Dilrukshi Herath, Aya C Taki, Nguyen Nghi, Jose Garcia-Bustos, Andreas Hofmann, Tao Wang, Guangxu Ma, Bill CH Chang, Abdul Jabbar, Brad E Sleebs, Robin B Gasser

Journal article  |  2020  |  MOLECULES

Kava extract, an aqueous rhizome emulsion of the plant Piper methysticum, has been used for centuries by Pacific Islanders as a ce..

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

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

Journal article  |  2020  |  EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Parasitic roundworms (nematodes) are significant pathogens of humans and animals and cause substantive socioeconomic losses due to..

Anti-Helicobacter pylori activity of ethoxzolamide.

Joyanta K Modak, Alexandra Tikhomirova, Rebecca J Gorrell, Mohammad M Rahman, Despina Kotsanas, Tony M Korman, Jose Garcia-Bustos, Terry Kwok, Richard L Ferrero, Claudiu T Supuran, Anna Roujeinikova

Journal article  |  2019  |  Journal of Enzyme Inhibition and Medicinal Chemistry

Ethoxzolamide (EZA), acetazolamide, and methazolamide are clinically used sulphonamide drugs designed to treat non-bacteria-relate..

An appraisal of natural products active against parasitic nematodes of animals

Jose F Garcia-Bustos, Brad E Sleebs, Robin B Gasser

Journal article  |  2019  |  PARASITES & VECTORS

Here, the scientific and patent literature on the activities of purified natural compounds has been reviewed, with the aim of asse..

Selected alpha-pyrones from the plants Cryptocarya novoguineensis (Lauraceae) and Piper methysticum (Piperaceae) with activity against Haemonchus contortus in vitro

HMP Dilrukshi Herath, Sarah Preston, Abdul Jabbar, Jose Garcia-Bustos, Russell S Addison, Sasha Hayes, Topul Rali, Tao Wang, Anson Koehler, Bill CH Chang, Andreas Hofmann, Rohan A Davis, Robin B Gasser

Journal article  |  2019  |  INTERNATIONAL JOURNAL FOR PARASITOLOGY-DRUGS AND DRUG RESISTANCE

Due to the widespread occurrence and spread of anthelmintic resistance, there is a need to develop new drugs against resistant par..

Tetrahydroquinoxalines induce a lethal evisceration phenotype in Haemonchus contortus in vitro

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

Journal article  |  2019  |  INTERNATIONAL JOURNAL FOR PARASITOLOGY-DRUGS AND DRUG RESISTANCE

In the present study, the anthelmintic activity of a human tyrosine kinase inhibitor, AG-1295, and 14 related tetrahydroquinoxalin..

Novel 1-Methyl-1H-pyrazole-5-carboxamide Derivatives with Potent Anthelmintic Activity

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

Journal article  |  2019  |  Journal of Medicinal Chemistry

A phenotypic screen of two different libraries of small molecules against the motility and development of the parasitic nematode H..