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List of works by Ian H. Gilbert

2,4-Diamino-6-methylpyrimidines for the potential treatment of Chagas' disease

scientific article published on 03 August 2018

2,4-Diaminopyrimidines as inhibitors of Leishmanial and Trypanosomal dihydrofolate reductase

scientific article published in November 2003

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)

A platform for target prediction of phenotypic screening hit molecules

scientific article published on 24 October 2019

Acetazolamide-based fungal chitinase inhibitors

scientific article

Acyclic Nucleoside Analogues as Inhibitors ofPlasmodiumfalciparumdUTPase

scientific article published on 01 July 2006

Alterations on the growth and ultrastructure of Leishmania chagasi induced by squalene synthase inhibitors

scientific article published on 23 March 2007

Amide bond replacements : incorporation of a 2,5,5-trisubstituted imidazoline into dipeptides and into a CCK-4 derivative

An approach to use an unusual adenosine transporter to selectively deliver polyamine analogues to trypanosomes

scientific article published on 01 April 1998

Analogues of thiolactomycin as potential anti-malarial and anti-trypanosomal agents

scientific article published in February 2004

Analogues of thiolactomycin as potential antimalarial agents

scientific article published on September 2005

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

Antiplasmodial activity of a series of 1,3,5-triazine-substituted polyamines.

scientific article published on July 2003

Antitrypanosomal 8-Hydroxy-Naphthyridines Are Chelators of Divalent Transition Metals

scholarly article by Richard J Wall et al published August 2018 in Antimicrobial Agents and Chemotherapy

Application of RNAi to Genomic Drug Target Validation in Schistosomes

scientific article

Application of a novel regulatable Cre recombinase system to define the role of liver and gut metabolism in drug oral bioavailability.

scientific article published in February 2015

Aryl phosphoramidates of 5-phospho erythronohydroxamic acid, a new class of potent trypanocidal compounds

scientific article

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

scientific article published on 01 November 2018

Automated design of ligands to polypharmacological profiles.

scientific article

Azasterols as inhibitors of sterol 24-methyltransferase in Leishmania species and Trypanosoma cruzi.

scientific article published in October 2003

Azasterols impair Giardia lamblia proliferation and induces encystation

scientific article published on 10 September 2007

Biochemical and Structural Characterization of Selective Allosteric Inhibitors of the Plasmodium falciparum Drug Target, Prolyl-tRNA-synthetase

scientific article

Challenges and recent progress in drug discovery for tropical diseases

scientific article published in Nature

Characterising covalent warhead reactivity.

scientific article published on 3 April 2019

Characterization of a melamino nitroheterocycle as a potential lead for the treatment of human african trypanosomiasis

scientific article

Chemical Validation of Methionyl-tRNA Synthetase as a Druggable Target in Leishmania donovani

scientific article published on 2 October 2017

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

scientific article

Clinical and veterinary trypanocidal benzoxaboroles target CPSF3

article published in the Proceedings of the National Academy of Sciences of the United States of America

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

scientific article published on 9 April 2013

Compounds enhancing human sperm motility identified using a high-throughput phenotypic screening platform

scientific article published on 07 January 2022

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

scientific article published on 25 May 2016

Crystal structures of a bacterial 6-phosphogluconate dehydrogenase reveal aspects of specificity, mechanism and mode of inhibition by analogues of high-energy reaction intermediates

scientific article

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

scientific article published in Nature

Deoxyuridine triphosphate nucleotidohydrolase as a potential antiparasitic drug target

scientific article published in September 2005

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

scientific article published on 10 November 2017

Design and preparation of sterol mimetics as potential antiparasitics

scientific article published on 9 August 2010

Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites

scientific article published on August 2005

Design and synthesis of bio-isosteres of thymidine triphosphate

scientific article published on 01 May 1998

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

Design, synthesis and evaluation of 2,4-diaminoquinazolines as inhibitors of trypanosomal and leishmanial dihydrofolate reductase.

scientific article

Design, synthesis and evaluation of novel uracil acetamide derivatives as potential inhibitors of Plasmodium falciparum dUTP nucleotidohydrolase.

scientific article published on 10 July 2008

Design, synthesis and evaluation of novel uracil amino acid conjugates for the inhibition of Trypanosoma cruzi dUTPase.

scientific article

Design, synthesis and evaluation of peptide libraries as potential anti-HIV compounds, via inhibition of gp120/cell membrane interactions, using the gp120/cd4/fab17 crystal structure

scientific article published on November 2002

Design, synthesis and evaluation of potential inhibitors of HIV gp120-CD4 interactions

scientific article published in May 2004

Design, synthesis, and evaluation of 5'-diphenyl nucleoside analogues as inhibitors of the Plasmodium falciparum dUTPase

scientific article

Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase

scientific article published in October 1999

Development of Chemical Proteomics for the Folateome and Analysis of the Kinetoplastid Folateome

article

Development of Small-Molecule Trypanosoma brucei N-Myristoyltransferase Inhibitors: Discovery and Optimisation of a Novel Binding Mode.

scientific article published on 23 September 2015

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 and Optimization of a Compound Series Active against Trypanosoma cruzi, the Causative Agent of Chagas Disease

scientific article published on 05 March 2020

Discovery and optimisation studies of antimalarial phenotypic hits.

scientific article published on 9 September 2015

Discovery and structure-activity relationships of pyrrolone antimalarials

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

Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.

scientific article

Drug discovery for neglected diseases: molecular target-based and phenotypic approaches

scientific article published on 09 September 2013

Effects of Inhibitors of [Delta]24(25)-Sterol Methyl Transferase on the Ultrastructure of Epimastigotes of Trypanosoma cruzi

scientific article published on 01 December 2005

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

Evaluation of azasterols as anti-parasitics.

scientific article published in October 2006

Evaluation of three novel azasterols against Toxoplasma gondii

scientific article published in December 2010

Exploring new inhibitors of Plasmodium falciparum purine nucleoside phosphorylase.

scientific article published on 14 August 2010

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

scientific article (publication date: 2013)

Finding new hits in neglected disease projects: target or phenotypic based screening?

scientific article published on January 2011

Fragment library design, synthesis and expansion: nurturing a synthesis and training platform

scientific article published on 25 October 2016

Fragment screening reveals salicylic hydroxamic acid as an inhibitor of Trypanosoma brucei GPI GlcNAc-PI de-N-acetylase.

scientific article published on 30 December 2013

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

Handling uncertainty in dynamic models: the pentose phosphate pathway in Trypanosoma brucei

scientific article (publication date: 2013)

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 a Proteasome-Targeting Arylsulfonamide with Potential for the Treatment of Chagas' Disease

scientific article published on 04 October 2021

Identification of inhibitors of an unconventional Trypanosoma brucei kinetochore kinase.

scientific article published in January 2019

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

scientific article published on 13 September 2011

Improved tricyclic inhibitors of trypanothione reductase by screening and chemical synthesis

scientific article

In vitro cell-free conversion of bacterial recombinant PrP to PrPres as a model for conversion

scientific article published in April 2003

Inhibitors of Trypanosoma brucei 6-Phosphogluconate Dehydrogenase

Inhibitors of dihydrofolate reductase in Leishmania and trypanosomes

scientific article

Interaction of monobenzamidine-linked trypanocides with the Trypanosoma brucei P2 aminopurine transporter

scientific article

Investigation of acyclic uridine amide and 5'-amido nucleoside analogues as potential inhibitors of the Plasmodium falciparum dUTPase.

scientific article published on 12 July 2013

Investigation of copper(II) tetrafluoroborate catalysed epoxide opening

scientific article published on December 2011

Investigation of trypanothione reductase as a drug target in Trypanosoma brucei

scientific article

Kinetic characterization of squalene synthase from Trypanosoma cruzi: selective inhibition by quinuclidine derivatives

scientific article published on 19 March 2007

Kinetic properties and inhibition of the dimeric dUTPase-dUDPase from Campylobacter jejuni

scientific article published on 01 February 2009

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

Mechanistic insights into the cure of prion disease by novel antiprion compounds

scientific article

Modified 5'-trityl nucleosides as inhibitors of Plasmodium falciparum dUTPase

scientific article published on 18 January 2011

Molecular dynamics simulations of wild-type and point mutation human prion protein at normal and elevated temperature

article

Multiple unbiased approaches identify oxidosqualene cyclase as the molecular target of a promising anti-leishmanial

scientific article published on 09 March 2021

N-(2-hydroxypropyl)methacrylamide-amphotericin B (HPMA-AmB) copolymer conjugates as antileishmanial agents

scientific article published on 20 December 2008

N-myristoyltransferase inhibitors as new leads to treat sleeping sickness

scientific article

N-myristoyltransferase is a cell wall target in Aspergillus fumigatus

scientific article published on 27 February 2015

New azasterols against Trypanosoma brucei: role of 24-sterol methyltransferase in inhibitor action.

scientific article

Nitrile reduction in the presence of Boc-protected amino groups by catalytic hydrogenation over palladium-activated Raney-nickel

scientific article

Novel azasterols as potential agents for treatment of leishmaniasis and trypanosomiasis.

scientific article published on August 2004

Novel functionalized melamine-based nitroheterocycles: synthesis and activity against trypanosomatid parasites

scientific article

Novel inhibitors of Leishmanial dihydrofolate reductase.

scientific article published in April 2001

Novel inhibitors of Trypanosoma cruzi dihydrofolate reductase.

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

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

Potential application of thymidylate kinase in nucleoside analogue activation in Plasmodium falciparum.

scientific article published on 6 August 2010

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

scientific article published on 08 April 2019

Preparation of transition-state analogues of sterol 24-methyl transferase as potential anti-parasitics.

scientific article published in September 2005

Probing the substrate specificity of Trypanosoma brucei GlcNAc-PI de-N-acetylase with synthetic substrate analogues.

scientific article

Quinol derivatives as potential trypanocidal agents

scientific article published on 27 December 2011

Quinuclidine derivatives as potential antiparasitics

scientific article

Rapid and sensitive quantitation of antibiotics in fermentations by electrospray mass spectrometry

article

SAR studies on azasterols as potential anti-trypanosomal and anti-leishmanial agents

scientific article published on 3 July 2009

Screening a protein kinase inhibitor library against Plasmodium falciparum

scientific article published on 7 November 2017

Selective delivery of 2-hydroxy APA to Trypanosoma brucei using the melamine motif

scientific article

Selective inhibition of 6-phosphogluconate dehydrogenase from Trypanosoma brucei.

scientific article published in May 2001

Selective inhibition of Trypanosoma brucei 6-phosphogluconate dehydrogenase by high-energy intermediate and transition-state analogues

scientific article

Setting Our Sights on Infectious Diseases

scientific article published on 06 December 2019

Site-directed mutagenesis provides insights into the selective binding of trityl derivatives to Plasmodium falciparum dUTPase

scientific article

Solid-phase synthesis of diamine and polyamine amino acid derivatives as HIV-1 tat-TAR binding inhibitors

scientific article published on January 2003

Squalamine analogues as potential anti-trypanosomal and anti-leishmanial compounds

scientific article published in 2000

Structural basis for the efficient phosphorylation of AZT-MP (3'-azido-3'-deoxythymidine monophosphate) and dGMP by Plasmodium falciparum type I thymidylate kinase

scientific article

Structure-activity relationship studies of pyrrolone antimalarial agents

scientific article published on 05 August 2013

Substituted Aminoacetamides as Novel Leads for Malaria Treatment

scientific article published on 03 July 2019

Synthesis and Evaluation of α-Thymidine Analogues as Novel Antimalarials

scientific article

Synthesis and biological evaluation of phosphate prodrugs of 4-phospho-D-erythronohydroxamic acid, an inhibitor of 6-phosphogluconate dehydrogenase

scientific article

Synthesis and biological evaluation of s-triazine substituted polyamines as potential new anti-trypanosomal drugs.

scientific article

Synthesis and biological evaluation of substrate-based inhibitors of 6-phosphogluconate dehydrogenase as potential drugs against African trypanosomiasis

scientific article

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

scientific article

Synthesis and evaluation of analogues of Congo red as potential compounds against transmissible spongiform encephalopathies

scientific article published in June 2003

Synthesis and testing of 5-benzyl-2,4-diaminopyrimidines as potential inhibitors of leishmanial and trypanosomal dihydrofolate reductase

scientific article published in October 2002

Synthesis and testing of peptides for anti-prion activity

scientific article

Synthesis of (R)-2-methyl-4-deoxy and (R)-2-methyl-4,5-dideoxy analogues of 6-phosphogluconate as potential inhibitors of 6-phosphogluconate dehydrogenase

scientific article published in February 2003

Synthesis of a homochiral α,α-disubstituted α,β-diamino-acid

Synthesis of analogues of Congo red and evaluation of their anti-prion activity

scientific article

Synthesis of potential anti-HIV GP120 inhibitors using a lysine template

scientific article published in June 2002

Synthetic arylquinuclidine derivatives exhibit antifungal activity against Candida albicans, Candida tropicalis and Candida parapsilopsis

scientific article published on 21 January 2011

Target assessment for antiparasitic drug discovery

scientific article

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

scientific article

Target-based drug discovery for human African trypanosomiasis: selection of molecular target and chemical matter

scientific article published on 09 August 2013

Targeted delivery of compounds to Trypanosoma brucei using the melamine motif

scientific article published on 31 January 2009

Targeting of toxic compounds to the trypanosome's interior

scientific article

The Qi Site of Cytochrome b is a Promiscuous Drug Target in Trypanosoma cruzi and Leishmania donovani

scientific article published on 30 January 2020

The structure-based design and synthesis of selective inhibitors of Trypanosoma cruzi dihydrofolate reductase.

scientific article published on May 1999

Thiolactomycin analogues as potential anti-Toxoplasma gondii agents

scientific article published on 19 August 2009

Towards the sustainable discovery and development of new antibiotics

scientific article published in 2021

Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials

scientific article published on 17 June 2016

Trypanocidal activity of melamine-based nitroheterocycles

scientific article published on May 2004

Validation of N-myristoyltransferase as Potential Chemotherapeutic Target in Mammal-Dwelling Stages of Trypanosoma cruzi

scientific article

Virtual fragment screening for novel inhibitors of 6-phosphogluconate dehydrogenase.

scientific article

Water-soluble polymer-drug conjugates for combination chemotherapy against visceral leishmaniasis

scientific article

Whole organism high-content screening by label-free, image-based Bayesian classification for parasitic diseases

scientific article

dUTPase as a platform for antimalarial drug design: structural basis for the selectivity of a class of nucleoside inhibitors.

scientific article published in February 2005

β-Branched acyclic nucleoside analogues as inhibitors of Plasmodium falciparum dUTPase

scientific article

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