Identification of 2-Aryl-Quinolone Inhibitors of Cytochrome bd and Chemical Validation of Combination Strategies for Respiratory Inhibitors against Mycobacterium tuberculosis

Autor: Laura N. Jeffreys, Alison Ardrey, Taghreed A. Hafiz, Lauri-Anne Dyer, Ashley J. Warman, Nada Mosallam, Gemma L. Nixon, Nicholas E. Fisher, W. David Hong, Suet C. Leung, Ghaith Aljayyoussi, Jaclyn Bibby, Deepak V. Almeida, Paul J. Converse, Nader Fotouhi, Neil G. Berry, Eric L. Nuermberger, Anna M. Upton, Paul M. O’Neill, Stephen A. Ward, Giancarlo A. Biagini

Publikováno v: ACS Infectious Diseases. 9:221-238

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d7bcc98728afc2851b04165451a027f5
https://doi.org/10.1021/acsinfecdis.2c00283

Rational Design, Synthesis, and Biological Evaluation of Heterocyclic Quinolones Targeting the Respiratory Chain of Mycobacterium tuberculosis

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

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

Identification of Novel Antimalarial Chemotypes via Chemoinformatic Compound Selection Methods for a High-Throughput Screening Program against the Novel Malarial Target, PfNDH2: Increasing Hit Rate via Virtual Screening Methods

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

Identification, Design and Biological Evaluation of Bisaryl Quinolones Targeting Plasmodium falciparum Type II NADH:Quinone Oxidoreductase (PfNDH2)

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

Antitubercular pharmacodynamics of phenothiazines

Autor: Paul M. O'Neill, Teresa Rito, Nicholas Fisher, Giancarlo A. Biagini, Neil G. Berry, Darren M. Moss, Stephen A. Ward, Ashley J. Warman

Publikováno v: The Journal of antimicrobial chemotherapy. 68(4)

OBJECTIVES: Phenothiazines have been shown to exhibit in vitro and in vivo activity against Mycobacterium tuberculosis (Mtb) and multidrug-resistant Mtb. They are predicted to target the genetically validated respiratory chain component type II NADH:

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d4365f13cef5dfc6cb8eaba3271c7c9f
https://pubmed.ncbi.nlm.nih.gov/23228936