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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

Molecules (Basel, Switzerland), 2020-03, Vol.25 (6), p.1423

2020

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The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents

Bioorganic & medicinal chemistry letters, 2007-04, Vol.17 (8), p.2150-2155

2007

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5-Substituted 2-Aminopyridine C-Nucleosides as Protonated Cytidine Equivalents: Increasing Efficiency and Selectivity in DNA Triple-Helix Formation

Journal of the American Chemical Society, 1997-06, Vol.119 (24), p.5499-5511

1997

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3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel

Bioorganic & medicinal chemistry, 2019-04, Vol.27 (7), p.1292-1307

2019

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Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles

Bioorganic & medicinal chemistry, 2018-05, Vol.26 (8), p.1797-1809

2018

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Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline

Bioorganic & medicinal chemistry, 2019-04, Vol.27 (7), p.1283-1291

2019

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Synthesis and 1H, 13C and 15N NMR characterisation of substituted Pyrazolo[4,3-c]quinolines and related compounds

Tetrahedron, 2018-05, Vol.74 (22), p.2797-2806

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

Journal of medicinal chemistry, 2018-03, Vol.61 (6), p.2329-2352

2018

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Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology

Bioorganic & medicinal chemistry, 2020-01, Vol.28 (1), p.115213, Article 115213

2020

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Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units

Bioorganic & medicinal chemistry letters, 2017-12, Vol.27 (23), p.5190-5196

2017

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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

Journal of medicinal chemistry, 2016-03, Vol.59 (6), p.2530-2550

2016

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Synthesis and Structure–Activity Relationships for Extended Side Chain Analogues of the Antitubercular Drug (6 S )-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5 H -imidazo[2,1- b ][1,3]oxazine (PA-824)

Journal of medicinal chemistry, 2015-04, Vol.58 (7), p.3036-3059

2015

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(4R)-4-[(1R)-1,2-Dihydroxy-ethyl]-1-[(1R)-1-phenyl-ethyl]pyrrolidin-2-one

Acta crystallographica. Section E, Structure reports online, 2008-09, Vol.64 (Pt 9), p.o1851-o1851

2008

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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)

Journal of medicinal chemistry, 2010-01, Vol.53 (1), p.282-294

2010

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Synthesis and Structure−Activity Relationships of Aza- and Diazabiphenyl Analogues of the Antitubercular Drug (6 S )-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5 H -imidazo[2,1- b ][1,3]oxazine (PA-824)

Journal of medicinal chemistry, 2010-12, Vol.53 (23), p.8421-8439

2010

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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

Bioorganic & medicinal chemistry letters, 2017-06, Vol.27 (11), p.2583-2589

2017

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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)

Journal of medicinal chemistry, 2010-12, Vol.53 (23), p.8421-8439

2010

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6‑Cyano Analogues of Bedaquiline as Less Lipophilic and Potentially Safer Diarylquinolines for Tuberculosis

ACS medicinal chemistry letters, 2017-10, Vol.8 (10), p.1019-1024

2017

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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)

Journal of medicinal chemistry, 2011-10, Vol.54 (19), p.6563-6585

2011

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Synthesis and Structure−activity Relationships of Antitubercular 2-Nitroimidazooxazines Bearing Heterocyclic Side Chains

Journal of medicinal chemistry, 2010-01, Vol.53 (2), p.855-866

2010

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Synthesis and Structure–Activity Relationships of Varied Ether Linker Analogues of the Antitubercular Drug (6 S )-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5 H -imidazo[2,1- b ][1,3]oxazine (PA-824)

Journal of medicinal chemistry, 2011-10, Vol.54 (19), p.6563-6585

2011

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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)

Journal of medicinal chemistry, 2012-01, Vol.55 (1), p.312-326

2012

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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)

Journal of medicinal chemistry, 2009-02, Vol.52 (3), p.637-645

2009

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Tricyclic [1,2,4]Triazine 1,4-Dioxides As Hypoxia Selective Cytotoxins

Journal of medicinal chemistry, 2008-11, Vol.51 (21), p.6853-6865

2008

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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

The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents

5-Substituted 2-Aminopyridine C-Nucleosides as Protonated Cytidine Equivalents: Increasing Efficiency and Selectivity in DNA Triple-Helix Formation

3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel

Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles

Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline

Synthesis and 1H, 13C and 15N NMR characterisation of substituted Pyrazolo[4,3-c]quinolines and related compounds

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

Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology

Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units

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

Synthesis and Structure–Activity Relationships for Extended Side Chain Analogues of the Antitubercular Drug (6 S )-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5 H -imidazo[2,1- b ][1,3]oxazine (PA-824)

(4R)-4-[(1R)-1,2-Dihydroxy-ethyl]-1-[(1R)-1-phenyl-ethyl]pyrrolidin-2-one

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)

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

Synthesis and Structure−Activity Relationships of Aza- and Diazabiphenyl Analogues of the Antitubercular Drug (6 S )-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5 H -imidazo[2,1- b ][1,3]oxazine (PA-824)

6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]thiazoles: Facile synthesis and comparative appraisal against tuberculosis and neglected tropical diseases

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)

6‑Cyano Analogues of Bedaquiline as Less Lipophilic and Potentially Safer Diarylquinolines for Tuberculosis

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)

Synthesis and Structure−activity Relationships of Antitubercular 2-Nitroimidazooxazines Bearing Heterocyclic Side Chains

Synthesis and Structure–Activity Relationships of Varied Ether Linker Analogues of the Antitubercular Drug (6 S )-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5 H -imidazo[2,1- b ][1,3]oxazine (PA-824)

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)

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)

Tricyclic [1,2,4]Triazine 1,4-Dioxides As Hypoxia Selective Cytotoxins

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