List of works - Paul G. Wyatt

2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 2. Synthesis, chirality, and pharmacokinetics

scientific article

2-Mercapto-Quinazolinones as Inhibitors of Type II NADH Dehydrogenase and Mycobacterium tuberculosis: Structure-Activity Relationships, Mechanism of Action and Absorption, Distribution, Metabolism, and Excretion Characterization.

scientific article published on 9 March 2018

A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors

scientific article published on 12 September 2018

A novel multiple-stage antimalarial agent that inhibits protein synthesis

scientific article (publication date: 18 June 2015)

Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need

scientific article published on 27 February 2017

Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need

scientific article published on 05 June 2017

Antitubercular 2-Pyrazolylpyrimidinones: Structure-Activity Relationship and Mode-of-Action Studies

scientific article published on 04 January 2021

Antitumor quinol PMX464 is a cytocidal anti-trypanosomal inhibitor targeting trypanothione metabolism

scientific article published on 6 January 2011

Author Correction: Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need

scientific article published on 01 November 2018

Chemical proteomic analysis reveals the drugability of the kinome of Trypanosoma brucei.

scientific article published on 23 August 2012

Chemical validation of trypanothione synthetase: a potential drug target for human trypanosomiasis

scientific article

Comparison of a high-throughput high-content intracellular Leishmania donovani assay with an axenic amastigote assay

scientific article published on 9 April 2013

Corrigendum: A novel multiple-stage antimalarial agent that inhibits protein synthesis

scientific article published on 25 May 2016

Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis

scientific article published in Nature

De Novo Design of Protein Kinase Inhibitors by in Silico Identification of Hinge Region-Binding Fragments

scientific article

Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors.

scientific article published on 10 November 2017

Design, synthesis and biological evaluation of Trypanosoma brucei trypanothione synthetase inhibitors

scientific article

Design, synthesis and biological evaluation of novel inhibitors of Trypanosoma brucei pteridine reductase 1.

scientific article

Detection of ligands from a dynamic combinatorial library by X-ray crystallography.

scientific article published in September 2003

Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides

scientific article published on March 1998

Dihydroquinazolines as a Novel Class of Trypanosoma brucei Trypanothione Reductase Inhibitors: Discovery, Synthesis, and Characterization of their Binding Mode by Protein Crystallography

scientific article

Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi

scientific article

Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei

scientific article published on 29 September 2015

Discovery of Inhibitors of Trypanosoma brucei by Phenotypic Screening of a Focused Protein Kinase Library

scientific article published on 18 September 2015

Discovery of a Novel Class of Orally Active Trypanocidal N -Myristoyltransferase Inhibitors

scientific article

Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy

scientific article published on 10 September 2016

Drug Discovery in Academia- the third way?

scientific article (publication date: October 2010)

Editorial [Hot Topic: Progress in Neglected Disease Drug Discovery (Guest Editors: Andrew L. Hopkins & Paul G. Wyatt)]

scientific article published on 01 January 2011

Erratum for De Rycker et al., Comparison of a High-Throughput High-Content Intracellular Leishmania donovani Assay with an Axenic Amastigote Assay

scholarly article published in Antimicrobial Agents and Chemotherapy

Essential but not vulnerable: indazole sulfonamides targeting inosine monophosphate dehydrogenase as potential leads against Mycobacterium tuberculosis

scientific article

Exploring the Trypanosoma brucei Hsp83 potential as a target for structure guided drug design

scientific article (publication date: 2013)

Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity

scientific article

Fragment-based hit identification: thinking in 3D.

scientific article

From on-target to off-target activity: identification and optimisation of Trypanosoma brucei GSK3 inhibitors and their characterisation as anti-Trypanosoma brucei drug discovery lead molecules

scientific article

Identification and optimisation of a series of 8-hydroxy naphthyridines with potent in vitro antileishmanial activity: Initial SAR and assessment of in vivo activity

scientific article published on 14 July 2020

Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis

scientific article published on 20 December 2018

Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB

scientific article published on 26 July 2018

Identification of inhibitors of protein kinase B using fragment-based lead discovery

scientific article

Identification of inhibitors of the Leishmania cdc2-related protein kinase CRK3.

scientific article published on 13 September 2011

Identification of potent and selective oxytocin antagonists. Part 1: indole and benzofuran derivatives

scientific article (publication date: 20 May 2002)

Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives

scientific article

Investigation of trypanothione reductase as a drug target in Trypanosoma brucei

scientific article

Lead optimization of a pyrazole sulfonamide series of Trypanosoma brucei N-myristoyltransferase inhibitors: identification and evaluation of CNS penetrant compounds as potential treatments for stage 2 human African trypanosomiasis

scientific article

Lessons learnt from assembling screening libraries for drug discovery for neglected diseases

scientific article

Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis

scientific article published on 20 March 2019

N-myristoyltransferase inhibitors as new leads to treat sleeping sickness

scientific article

One Scaffold, Three Binding Modes: Novel and Selective Pteridine Reductase 1 Inhibitors Derived from Fragment Hits Discovered by Virtual Screening

scientific article

Optimisation of the anti-Trypanosoma brucei activity of the opioid agonist U50488

scientific article

PE/PPE proteins mediate nutrient transport across the outer membrane of Mycobacterium tuberculosis

scientific article published on 01 March 2020

Pharmacological Validation of N-Myristoyltransferase as a Drug Target in Leishmania donovani

scholarly article by Victoriano Corpas-Lopez et al published 12 November 2018 in ACS Infectious Diseases

Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition

scientific article published on 08 April 2019

Quinol derivatives as potential trypanocidal agents

scientific article published on 27 December 2011

Screening a protein kinase inhibitor library against Plasmodium falciparum

scientific article published on 7 November 2017

Screening of a Novel Fragment Library with Functional Complexity against Mycobacterium tuberculosis InhA.

scientific article published on 5 February 2018

Setting Our Sights on Infectious Diseases

scientific article published on 06 December 2019

Sialidase inhibitors related to zanamivir. Further SAR studies of 4-amino-4H-pyran-2-carboxylic acid-6-propylamides

scientific article

Structure-Activity Relationships of Pyrazolo[1,5-<i>a</i>]pyrimidin-7(4<i>H</i>)-ones as Antitubercular Agents

scientific article published on 06 January 2021

Structure-activity relationship studies of pyrrolone antimalarial agents

scientific article published on 05 August 2013

Synthesis and evaluation of 1-(1-(Benzo[b]thiophen-2-yl)cyclohexyl)piperidine (BTCP) analogues as inhibitors of trypanothione reductase

scientific article

Target assessment for antiparasitic drug discovery

scientific article

Target validation: linking target and chemical properties to desired product profile

scientific article

List of works by Paul G. Wyatt

2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 2. Synthesis, chirality, and pharmacokinetics

2-Mercapto-Quinazolinones as Inhibitors of Type II NADH Dehydrogenase and Mycobacterium tuberculosis: Structure-Activity Relationships, Mechanism of Action and Absorption, Distribution, Metabolism, and Excretion Characterization.

A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors

A novel multiple-stage antimalarial agent that inhibits protein synthesis

Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need

Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need

Antitubercular 2-Pyrazolylpyrimidinones: Structure-Activity Relationship and Mode-of-Action Studies

Antitumor quinol PMX464 is a cytocidal anti-trypanosomal inhibitor targeting trypanothione metabolism

Author Correction: Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need

Chemical proteomic analysis reveals the drugability of the kinome of Trypanosoma brucei.

Chemical validation of trypanothione synthetase: a potential drug target for human trypanosomiasis

Comparison of a high-throughput high-content intracellular Leishmania donovani assay with an axenic amastigote assay

Corrigendum: A novel multiple-stage antimalarial agent that inhibits protein synthesis

Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis

De Novo Design of Protein Kinase Inhibitors by in Silico Identification of Hinge Region-Binding Fragments

Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors.

Design, synthesis and biological evaluation of Trypanosoma brucei trypanothione synthetase inhibitors

Design, synthesis and biological evaluation of novel inhibitors of Trypanosoma brucei pteridine reductase 1.

Detection of ligands from a dynamic combinatorial library by X-ray crystallography.

Dihydropyrancarboxamides related to zanamivir: a new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides

Dihydroquinazolines as a Novel Class of Trypanosoma brucei Trypanothione Reductase Inhibitors: Discovery, Synthesis, and Characterization of their Binding Mode by Protein Crystallography

Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi

Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei

Discovery of Inhibitors of Trypanosoma brucei by Phenotypic Screening of a Focused Protein Kinase Library

Discovery of a Novel Class of Orally Active Trypanocidal N -Myristoyltransferase Inhibitors

Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy

Drug Discovery in Academia- the third way?

Editorial [Hot Topic: Progress in Neglected Disease Drug Discovery (Guest Editors: Andrew L. Hopkins & Paul G. Wyatt)]

Erratum for De Rycker et al., Comparison of a High-Throughput High-Content Intracellular Leishmania donovani Assay with an Axenic Amastigote Assay

Essential but not vulnerable: indazole sulfonamides targeting inosine monophosphate dehydrogenase as potential leads against Mycobacterium tuberculosis

Exploring the Trypanosoma brucei Hsp83 potential as a target for structure guided drug design

Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity

Fragment-based hit identification: thinking in 3D.

From on-target to off-target activity: identification and optimisation of Trypanosoma brucei GSK3 inhibitors and their characterisation as anti-Trypanosoma brucei drug discovery lead molecules

Identification and optimisation of a series of 8-hydroxy naphthyridines with potent in vitro antileishmanial activity: Initial SAR and assessment of in vivo activity

Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis

Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB

Identification of inhibitors of protein kinase B using fragment-based lead discovery

Identification of inhibitors of the Leishmania cdc2-related protein kinase CRK3.

Identification of potent and selective oxytocin antagonists. Part 1: indole and benzofuran derivatives

Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives

Investigation of trypanothione reductase as a drug target in Trypanosoma brucei

Lead optimization of a pyrazole sulfonamide series of Trypanosoma brucei N-myristoyltransferase inhibitors: identification and evaluation of CNS penetrant compounds as potential treatments for stage 2 human African trypanosomiasis

Lessons learnt from assembling screening libraries for drug discovery for neglected diseases

Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis

N-myristoyltransferase inhibitors as new leads to treat sleeping sickness

One Scaffold, Three Binding Modes: Novel and Selective Pteridine Reductase 1 Inhibitors Derived from Fragment Hits Discovered by Virtual Screening

Optimisation of the anti-Trypanosoma brucei activity of the opioid agonist U50488

PE/PPE proteins mediate nutrient transport across the outer membrane of Mycobacterium tuberculosis

Pharmacological Validation of N-Myristoyltransferase as a Drug Target in Leishmania donovani

Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition

Quinol derivatives as potential trypanocidal agents

Screening a protein kinase inhibitor library against Plasmodium falciparum

Screening of a Novel Fragment Library with Functional Complexity against Mycobacterium tuberculosis InhA.

Setting Our Sights on Infectious Diseases

Sialidase inhibitors related to zanamivir. Further SAR studies of 4-amino-4H-pyran-2-carboxylic acid-6-propylamides

Structure-Activity Relationships of Pyrazolo[1,5-<i>a</i>]pyrimidin-7(4<i>H</i>)-ones as Antitubercular Agents

Structure-activity relationship studies of pyrrolone antimalarial agents

Synthesis and evaluation of 1-(1-(Benzo[b]thiophen-2-yl)cyclohexyl)piperidine (BTCP) analogues as inhibitors of trypanothione reductase

Target assessment for antiparasitic drug discovery

Target validation: linking target and chemical properties to desired product profile