Small molecule inhibitors of the LEDGF site of human immunodeficiency virus integrase identified by fragment screening and structure based design.

Autor: Thomas S Peat, David I Rhodes, Nick Vandegraaff, Giang Le, Jessica A Smith, Lisa J Clark, Eric D Jones, Jonathan A V Coates, Neeranat Thienthong, Janet Newman, Olan Dolezal, Roger Mulder, John H Ryan, G Paul Savage, Craig L Francis, John J Deadman

Publikováno v: PLoS ONE, Vol 7, Iss 7, p e40147 (2012)

A fragment-based screen against human immunodeficiency virus type 1 (HIV) integrase led to a number of compounds that bound to the lens epithelium derived growth factor (LEDGF) binding site of the integrase catalytic core domain. We determined the cr

Externí odkaz: https://doaj.org/article/00a299504a0c4c219911a597e18decce

A Subset Screen of the Compounds Australia Scaffold Library Identifies 7-Acylaminodibenzoxazepinones as Potent and Selective Hits for Anti-Giardia Drug Discovery

Autor: Christopher J. S. Hart, Andrew G. Riches, Snigdha Tiash, Erin Clapper, Soumya Ramu, Johannes Zuegg, John H. Ryan, Tina S. Skinner-Adams

Publikováno v: Biomedicines, Vol 10, Iss 12, p 3182 (2022)

On an annual basis the flagellate protozoan, Giardia duodenalis, is responsible for an estimated one billion human infections of which approximately two hundred million cause disease. However, the treatment of Giardia infections is reliant on a small

Externí odkaz: https://doaj.org/article/4f6dd0a1bdf549999d1439e7cc7483e9

Discovery of 1,3,4-oxadiazoles with slow-action activity againstPlasmodium falciparummalaria parasites

Autor: Katherine T. Andrews, Gillian M. Fisher, Meaghan Firmin, Andris J. Liepa, Tony Wilson, James Gardiner, Yacine Mohri, Anjana Rai, Andrew K. Davey, Antoine Masurier, Alix Delion, Alexandos A. Mouratidis, Oliver Hutt, Jeremy N. Burrows, John H. Ryan, Andrew G. Riches, Tina S. Skinner-Adams

To achieve malaria eradication, new preventative agents that act differently to front-line treatment drugs are needed. To identify potential chemoprevention starting points we screened a sub-set of the CSIRO Australia Compound Collection for compound

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c5f71c16c50f3313b0dd97d54fc96a3e
https://doi.org/10.1101/2023.03.09.531229

The preparation of novel histrionicotoxin analogues and their activity towards the α4β2 and α7 nicotinic acetylcholine receptors

Autor: Michael Sako, John H. Ryan, Simon Saubern, Mary Chebib, James M. MacDonald, Cecily Eldridge, Gracia X. J. Quek

Publikováno v: Tetrahedron. 74:1245-1252

Four histrionicotoxin analogues were prepared in an efficient manner utilizing a nitrone dipolar cycloaddition reaction as the key step in forming tricyclic intermediate 13. The nitrile in intermediate 13 was reduced with DIBAL to an aldehyde which t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e944840d99955cf263da79b350f68542
https://doi.org/10.1016/j.tet.2017.11.047

A novel in vitro image-based assay identifies new drug leads for giardiasis

Autor: Andrew G. Riches, John H. Ryan, Katherine T. Andrews, Christopher J.S. Hart, Tina S. Skinner-Adams, Taylah Munro

Publikováno v: International Journal for Parasitology: Drugs and Drug Resistance, Vol 7, Iss 1, Pp 83-89 (2017)
International Journal for Parasitology: Drugs and Drug Resistance

Giardia duodenalis is an intestinal parasite that causes giardiasis, a widespread human gastrointestinal disease. Treatment of giardiasis relies on a small arsenal of compounds that can suffer from limitations including side-effects, variable treatme

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e29d0f7c263bf0ad35fcbd7c66f504fd
http://www.sciencedirect.com/science/article/pii/S2211320716301300