Publications by authors named "Brian D Palmer"

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Synthesis and Structure-Activity Relationships for the Anti-Mycobacterial Activity of 3-Phenyl--(Pyridin-2-ylmethyl)Pyrazolo[1,5-]Pyrimidin-7-Amines.
Hamish S Sutherland, Peter J Choi, Guo-Liang Lu, Anna C Giddens, Amy S T Tong, Brian D Palmer

Pharmaceuticals (Basel)· September 2022

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Evaluation of Novel Inhibitors of Tryptophan Dioxygenases for Enzyme and Species Selectivity Using Engineered Tumour Cell Lines Expressing Either Murine or Human IDO1 or TDO2.
Sofian M Tijono, Brian D Palmer, Petr Tomek, Jack U Flanagan, Kimiora Henare

Pharmaceuticals (Basel)· August 2022

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Synthesis and structure-activity relationships for a new class of tetrahydronaphthalene amide inhibitors of Mycobacterium tuberculosis.
Hamish S Sutherland, Guo-Liang Lu, Amy S T Tong, Daniel Conole, Scott G Franzblau, Brian D Palmer

Eur J Med Chem· February 2022

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Synthetic studies towards isomeric pyrazolopyrimidines as potential ATP synthesis inhibitors of . Structural correction of reported -(6-(2-(dimethylamino)ethoxy)-5-fluoropyridin-3-yl)-2-(4-fluorophenyl)-5-(trifluoromethyl)pyrazolo[1,5-]pyrimidin-7-amine.
Peter J Choi, Guo-Liang Lu, Hamish S Sutherland, Anna C Giddens, Scott G Franzblau, Brian D Palmer

Tetrahedron Lett· February 2022

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Parallel discovery of selective and dual inhibitors of tryptophan dioxygenases IDO1 and TDO2 with a newly-modified enzymatic assay.
Rossella Capochiani de Iudicibus, Petr Tomek, Brian D Palmer, Sofian M Tijono, Jack U Flanagan

Bioorg Med Chem· June 2021

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Synthesis and structure-activity relationships for tetrahydroisoquinoline-based inhibitors of Mycobacterium tuberculosis.
Guo-Liang Lu, Amy S T Tong, Daniel Conole, Hamish S Sutherland, Peter J Choi, Brian D Palmer

Bioorg Med Chem· November 2020

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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, Brian D Palmer

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, Brian D Palmer

Bioorg Med Chem· January 2020

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Dual pH-sensitive liposomes with low pH-triggered sheddable PEG for enhanced tumor-targeted drug delivery.
Manju Kanamala, Brian D Palmer, Stephen Mf Jamieson, William R Wilson, Zimei Wu

Nanomedicine (Lond)· August 2019

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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, Brian D Palmer

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, Brian D Palmer

Bioorg Med Chem· April 2019

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Characterization of a smart pH-cleavable PEG polymer towards the development of dual pH-sensitive liposomes.
Manju Kanamala, Brian D Palmer, William R Wilson, Zimei Wu

Int J Pharm· September 2018

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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, Brian D Palmer

Bioorg Med Chem· May 2018

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PEG-Benzaldehyde-Hydrazone-Lipid Based PEG-Sheddable pH-Sensitive Liposomes: Abilities for Endosomal Escape and Long Circulation.
Manju Kanamala, Brian D Palmer, Hamidreza Ghandehari, William R Wilson, Zimei Wu

Pharm Res· May 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, Brian D Palmer

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, Brian D Palmer

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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Discovery and evaluation of inhibitors to the immunosuppressive enzyme indoleamine 2,3-dioxygenase 1 (IDO1): Probing the active site-inhibitor interactions.
Petr Tomek, Brian D Palmer, Jack U Flanagan, Chuanwen Sun, Emma L Raven

Eur J Med Chem· January 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, Brian D Palmer

J Med Chem· September 2016

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Mechanisms and biomaterials in pH-responsive tumour targeted drug delivery: A review.
Manju Kanamala, William R Wilson, Mimi Yang, Brian D Palmer, Zimei Wu

Biomaterials· April 2016

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Formation of fluorophores from the kynurenine pathway metabolite N-formylkynurenine and cyclic amines involves transamidation and carbon-carbon bond formation at the 2-position of the amine.
Petr Tomek, Brian D Palmer, Jackie D Kendall, Jack U Flanagan, Lai-Ming Ching

Biochim Biophys Acta· September 2015

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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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Discovery and characterisation of hydrazines as inhibitors of the immune suppressive enzyme, indoleamine 2,3-dioxygenase 1 (IDO1).
Sai-Parng S Fung, Haiyan Wang, Petr Tomek, Christopher J Squire, Jack U Flanagan, Brian D Palmer

Bioorg Med Chem· December 2013

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Formation of an N-formylkynurenine-derived fluorophore and its use for measuring indoleamine 2,3-dioxygenase 1 activity.
Petr Tomek, Brian D Palmer, Jack U Flanagan, Sai-Parng S Fung, David J A Bridewell

Anal Bioanal Chem· March 2013

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