Zobrazeno 1 - 10
of 42
pro vyhledávání: '"Paul A. Stocks"'
Autor:
Nicholas Fisher, Ghaith Aljayyoussi, Paul M. O'Neill, Maria Lurdes Santos Cristiano, Peter Gibbons, Ashley J. Warman, Richard Amewu, W. David Hong, Gemma L. Nixon, Neil G. Berry, Giancarlo A. Biagini, Stephen A. Ward, Maxine Caws, Andrew V. Stachulski, Raman Sharma, Darren M. Moss, Sally Mead, Paul A. Stocks, Alison E. Shone, Pedro Horta, Alison Ardrey, Paul T. P. Bedingfield, Suet C. Leung
Publikováno v:
Journal of medicinal chemistry
Repositório Científico de Acesso Aberto de Portugal
Repositório Científico de Acesso Aberto de Portugal (RCAAP)
instacron:RCAAP
Repositório Científico de Acesso Aberto de Portugal
Repositório Científico de Acesso Aberto de Portugal (RCAAP)
instacron:RCAAP
A high-throughput screen (HTS) was undertaken against the respiratory chain dehydrogenase component, NADH:menaquinone oxidoreductase (Ndh) of Mycobacterium tuberculosis (Mtb). The 11000 compounds were selected for the HTS based on the known phenothia
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::75eea3deff75a8df20d74c3435238d4b
Autor:
Paul M. O'Neill, Alison Mbekeani, Janet Hemingway, Giancarlo A. Biagini, Neil G. Berry, Alison E. Shone, Richard Amewu, Michael J. Delves, Bénédicte Pacorel, Nicholas Fisher, Chandrakala Pidathala, Suet C. Leung, David W. Hong, Robert E. Sinden, James Chadwick, Jill Davies, Murad A. Mubaraki, Gemma L. Nixon, Raman Sharma, Thomas Antoine, Stephen A. Ward, Alisdair Hill, Alexandre S. Lawrenson, Sitthivut Charoensutthivarakul, Abhishek Srivastava, Olivier Berger, Clemens H. M. Kocken, Lee Taylor, Ashley J. Warman, Paul A. Stocks, Anne-Marie Zeeman, Peter Gibbons
Publikováno v:
Proceedings of the National Academy of Sciences. 109:8298-8303
There is an urgent need for new antimalarial drugs with novel mechanisms of action to deliver effective control and eradication programs. Parasite resistance to all existing antimalarial classes, including the artemisinins, has been reported during t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::72e4fc34ad06f807aeeaf6df13dc85ca
https://doi.org/10.1073/pnas.1205651109
https://doi.org/10.1073/pnas.1205651109
Autor:
Alasdair Hill, Peter Gibbons, Alison E. Shone, David William Cronk, Gemma L. Nixon, Stephen A. Ward, Chandrakala Pidathala, David W. Hong, Ian K. Gowers, Richard Amewu, Alison Mbekeani, Raman Sharma, Joanne Lesley Shearer, Serge P. Parel, Alexandre S. Lawrenson, Giancarlo A. Biagini, Paul A. Stocks, Ashley J. Warman, Paul M. O'Neill, Suet C. Leung, James Chadwick, Nicholas Fisher, Neil G. Berry
Publikováno v:
Journal of Medicinal Chemistry
Malaria is responsible for approximately 1 million deaths annually; thus, continued efforts to discover new antimalarials are required. A HTS screen was established to identify novel inhibitors of the parasite's mitochondrial enzyme NADH:quinone oxid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7a92ac08cbafc0496b020e0ff8983755
https://doi.org/10.1021/jm3001482
https://doi.org/10.1021/jm3001482
Autor:
Suet C. Leung, Peter Gibbons, Richard Amewu, Gemma L. Nixon, Chandrakala Pidathala, W. David Hong, Bénédicte Pacorel, Neil G. Berry, Raman Sharma, Paul A. Stocks, Abhishek Srivastava, Alison E. Shone, Sitthivut Charoensutthivarakul, Lee Taylor, Olivier Berger, Alison Mbekeani, Alasdair Hill, Nicholas E. Fisher, Ashley J. Warman, Giancarlo A. Biagini, Stephen A. Ward, Paul M. O’Neill
Publikováno v:
Journal of Medicinal Chemistry
Following a program undertaken to identify hit compounds against NADH:ubiquinone oxidoreductase (PfNDH2), a novel enzyme target within the malaria parasite Plasmodium falciparum, hit to lead optimization led to identification of CK-2-68, a molecule s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78aa7833101752871927baf4ebe23ca0
https://doi.org/10.1021/jm201184h
https://doi.org/10.1021/jm201184h
Autor:
Abhishek Srivastava, Suet C. Leung, Neil G. Berry, Paul M. O'Neill, Richard Amewu, Alison Mbekeani, Alison E. Shone, Olivier Berger, Gemma L. Nixon, Sitthivut Charoensutthivarakul, Stephen A. Ward, Paul A. Stocks, W. David Hong, Bénédicte Pacorel, Alasdair Hill, Nicholas Fisher, Raman Sharma, Chandrakala Pidathala, Peter Gibbons, Giancarlo A. Biagini, Lee Taylor, Ashley J. Warman
Publikováno v:
Journal of Medicinal Chemistry
A program was undertaken to identify hit compounds against NADH:ubiquinone oxidoreductase (PfNDH2), a dehydrogenase of the mitochondrial electron transport chain of the malaria parasite Plasmodium falciparum. PfNDH2 has only one known inhibitor, hydr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3354d09c794a80f97f6dcf740bfec51d
http://europepmc.org/articles/PMC3297363
http://europepmc.org/articles/PMC3297363
Autor:
Sanjeev Krishna, David J. Johnson, Stephen A. Ward, Alexis Nzila, Edwin Ochong, Susan Beveridge, Paul M. O'Neill, J. Enrique Salcedo-Sora, Giancarlo A. Biagini, Patrick G. Bray, Paul A. Stocks
Publikováno v:
The Journal of Biological Chemistry
Background: Antifolates have been effective antimalarial drugs. Results: Two proteins of P. falciparum facilitate membrane transport of folates but also of pABA, a precursor of folates. Conclusion: At the concentration that pABA is in the human plasm
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ad7f80a01aa15752a0f1024ae1e02f51
http://europepmc.org/articles/PMC3247980
http://europepmc.org/articles/PMC3247980
Autor:
Neil G. Berry, Donatella Taramelli, Sergio Wittlin, Paul M. O'Neill, Hollie Burrell-Saward, Fatima Bousejra-El Garah, James Chadwick, Matthias Rottmann, Paul A. Stocks, Richard Amewu, Reto Brun, Raman Sharma, Stephen A. Ward, Silvia Parapini, Francesc Marti
Publikováno v:
ChemMedChem. 6:1357-1361
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2bee657c95caf2553403136be37d4e5
https://doi.org/10.1002/cmdc.201100196
https://doi.org/10.1002/cmdc.201100196
Autor:
Jill Davies, Tafadzwa Charidza, Miriam E. Kennedy, B. Kevin Park, Amy E. Mercer, Ivo Piantanida, Michael Jones, Paul M. O'Neill, Jonathan Baird, Omar Janneh, Patrick G. Bray, Richard Cosstick, Paul A. Stocks, Sarah L. Rawe, Stephen A. Ward, Louise La Pensee
Publikováno v:
Articles
Artemisinin-acridine hybrids were prepared and evaluated for their in vitro activity against tumour cell lines and a chloroquine sensitive strain of Plasmodium falciparum. They showed a 2-4-fold increase in activity against HL60, MDA-MB-231 and MCF-7
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16dfc301f102ae95bee6407f88e87303
https://doi.org/10.1016/j.bmcl.2009.02.028
https://doi.org/10.1016/j.bmcl.2009.02.028
Autor:
Stephen Hindley, Paul M. O'Neill, Eghbaleh Asadollahy, Karen Rimmer, Alison E. Shone, Gemma L. Nixon, James L. Maggs, Stephen A. Ward, Richard A. Brigandi, Martin Bates, Patrick G. Bray, P. A. Winstanley, Paul A. Stocks, Jill Davies, Silvia Parapini, Livia Vivas, Domingo Gargallo, Stephanie L. Gresham, Hollie Lander, Giancarlo A. Biagini, B. Kevin Park, Donatella Taramelli, Ramesh Bambal, Federico M. Gomez-de-las-Heras, Charles B. Davis, Charlotte Hall, Neil G. Berry, Phil Roberts, Deborah Stanford
Publikováno v:
Journal of Medicinal Chemistry. 52:1828-1844
On the basis of a mechanistic understanding of the toxicity of the 4-aminoquinoline amodiaquine (1b), three series of amodiaquine analogues have been prepared where the 4-aminophenol "metabolic alert" has been modified by replacement of the 4'-hydrox
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::31d2075934bbaca76abf6a07eb93897a
https://doi.org/10.1021/jm8012757
https://doi.org/10.1021/jm8012757
Autor:
Stephanie L. Gresham, P. Roberts, Federico M. Gomez-de-las-Heras, Charles B. Davis, Timothy K. Hart, Ron M. Lawrence, Neil G. Berry, Paul M. O'Neill, Domingo Gargallo, B. Kevin Park, Stephen Hindley, Patrick G. Bray, Giancarlo A. Biagini, James L. Maggs, Amira Mukhtar, Peter Gibbons, P. A. Winstanley, Richard A. Brigandi, Paul A. Stocks, Alison E. Shone, Ramesh Bambal, Martin Bates, Richard P. Bonar-Law, Stephen A. Ward
Publikováno v:
Journal of Medicinal Chemistry. 52:1408-1415
N-tert-Butyl isoquine (4) (GSK369796) is a 4-aminoquinoline drug candidate selected and developed as part of a public-private partnership between academics at Liverpool, MMV, and GSK pharmaceuticals. This molecule was rationally designed based on che
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f35436c97f1a67b9100d3dc4b1c06355
https://doi.org/10.1021/jm8012618
https://doi.org/10.1021/jm8012618