Publications by authors named "Adrian Blaser"

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Synthetic Studies to Help Elucidate the Metabolism of the Preclinical Candidate TBAJ-876-A Less Toxic and More Potent Analogue of Bedaquiline.
Peter J Choi, Daniel Conole, Hamish S Sutherland, Adrian Blaser, Amy S T Tong

Molecules· March 2020

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Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.
Hamish S Sutherland, Amy S T Tong, Peter J Choi, Adrian Blaser, Scott G Franzblau

Bioorg Med Chem· January 2020

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Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.
Adrian Blaser, Hamish S Sutherland, Amy S T Tong, Peter J Choi, Daniel Conole

Bioorg Med Chem· April 2019

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3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.
Hamish S Sutherland, Amy S T Tong, Peter J Choi, Adrian Blaser, Daniel Conole

Bioorg Med Chem· April 2019

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Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.
Hamish S Sutherland, Amy S T Tong, Peter J Choi, Daniel Conole, Adrian Blaser

Bioorg Med Chem· May 2018

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Development of (6 R)-2-Nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5 H-imidazo[2,1- b][1,3]oxazine (DNDI-8219): A New Lead for Visceral Leishmaniasis.
Andrew M Thompson, Patrick D O'Connor, Andrew J Marshall, Adrian Blaser, Vanessa Yardley

J Med Chem· March 2018

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Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units.
Peter J Choi, Hamish S Sutherland, Amy S T Tong, Adrian Blaser, Scott G Franzblau

Bioorg Med Chem Lett· December 2017

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6-Cyano Analogues of Bedaquiline as Less Lipophilic and Potentially Safer Diarylquinolines for Tuberculosis.
Amy S T Tong, Peter J Choi, Adrian Blaser, Hamish S Sutherland, Sophia K Y Tsang

ACS Med Chem Lett· October 2017

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6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]thiazoles: Facile synthesis and comparative appraisal against tuberculosis and neglected tropical diseases.
Andrew M Thompson, Adrian Blaser, Brian D Palmer, Robert F Anderson, Sujata S Shinde

Bioorg Med Chem Lett· June 2017

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Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.
Jeff B Smaill, Andrea J Gonzales, Julie A Spicer, Helen Lee, Jessica E Reed, Adrian Blaser

J Med Chem· September 2016

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Repositioning Antitubercular 6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]oxazoles for Neglected Tropical Diseases: Structure-Activity Studies on a Preclinical Candidate for Visceral Leishmaniasis.
Andrew M Thompson, Patrick D O'Connor, Adrian Blaser, Vanessa Yardley, Louis Maes

J Med Chem· March 2016

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Biarylmethoxy 2-nitroimidazooxazine antituberculosis agents: Effects of proximal ring substitution and linker reversal on metabolism and efficacy.
Andrew M Thompson, Adrian Blaser, Brian D Palmer, Scott G Franzblau, Baojie Wan

Bioorg Med Chem Lett· September 2015

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Synthesis and structure-activity relationships for extended side chain analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824).
Brian D Palmer, Hamish S Sutherland, Adrian Blaser, Iveta Kmentova, Scott G Franzblau

J Med Chem· April 2015

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Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824).
Adrian Blaser, Brian D Palmer, Hamish S Sutherland, Iveta Kmentova, Scott G Franzblau

J Med Chem· January 2012

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Synthesis and structure-activity relationships of varied ether linker analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5h-imidazo[2,1-b][1,3]oxazine (PA-824).
Andrew M Thompson, Hamish S Sutherland, Brian D Palmer, Iveta Kmentova, Adrian Blaser

J Med Chem· October 2011

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Synthesis and structure-activity relationships of aza- and diazabiphenyl analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824).
Iveta Kmentova, Hamish S Sutherland, Brian D Palmer, Adrian Blaser, Scott G Franzblau

J Med Chem· December 2010

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Synthesis and structure-activity studies of biphenyl analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824).
Brian D Palmer, Andrew M Thompson, Hamish S Sutherland, Adrian Blaser, Iveta Kmentova

J Med Chem· January 2010

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Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains.
Hamish S Sutherland, Adrian Blaser, Iveta Kmentova, Scott G Franzblau, Baojie Wan

J Med Chem· January 2010

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Synthesis, reduction potentials, and antitubercular activity of ring A/B analogues of the bioreductive drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824).
Andrew M Thompson, Adrian Blaser, Robert F Anderson, Sujata S Shinde, Scott G Franzblau

J Med Chem· February 2009

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Tricyclic [1,2,4]triazine 1,4-dioxides as hypoxia selective cytotoxins.
Michael P Hay, Kevin O Hicks, Karin Pchalek, Ho H Lee, Adrian Blaser

J Med Chem· November 2008

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(4R)-4-[(1R)-1,2-Dihydroxy-ethyl]-1-[(1R)-1-phenyl-ethyl]pyrrolidin-2-one.
Adrian Blaser, Peter D W Boyd

Acta Crystallogr Sect E Struct Rep Online· August 2008

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The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents.
Sean T Murphy, Heather L Case, Edmund Ellsworth, Susan Hagen, Michael Huband, Adrian Blaser

Bioorg Med Chem Lett· April 2007

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