Shane R. Wilkinson
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View article: Bone measurements interact with phenotypic measures in canine Duchenne muscular dystrophy
Bone measurements interact with phenotypic measures in canine Duchenne muscular dystrophy Open
Duchenne muscular dystrophy (DMD) is an X-linked muscle disease with weakness, loss of ambulation, and premature death. DMD patients have reduced bone health, including decreased femur length (FL), density, and fractures. The mdx mouse mod…
View article: Systematic study of 1,2,3-triazolyl sterols for the development of new drugs against parasitic Neglected Tropical Diseases
Systematic study of 1,2,3-triazolyl sterols for the development of new drugs against parasitic Neglected Tropical Diseases Open
A series of thirty 1,2,3-triazolylsterols, inspired by azasterols with proven antiparasitic activity, were prepared by a stereocontrolled synthesis. Ten of these compounds constitute chimeras/hybrids of 22,26-azasterol (AZA) and 1,2,3-tria…
View article: Systematic study of triazolyl sterols for the development of new drugs against parasitic Neglected Tropical Diseases.
Systematic study of triazolyl sterols for the development of new drugs against parasitic Neglected Tropical Diseases. Open
A series of thirty 1,2,3-triazolylsterols, inspired by azasterols with proven antiparasitic activity, were prepared by a stereocontrolled synthesis. Ten of these compounds constitute chimeras/hybrids of AZA and 1,2,3-triazolyl azasterols. …
View article: Systematic study of triazolyl sterols for the development of new drugs against parasitic Neglected Tropical Diseases.
Systematic study of triazolyl sterols for the development of new drugs against parasitic Neglected Tropical Diseases. Open
A series of thirty 1,2,3-triazolylsterols were prepared by a stereocontrolled synthesis and inspired by azasterols with proven antiparasitic activity. Ten of these compounds constitute chimeras/hybrids of AZA and 1,2,3-triazolyl azasterols…
View article: Systematic study of triazolyl sterols for the development of new drugs against parasitic Neglected Tropical Diseases.
Systematic study of triazolyl sterols for the development of new drugs against parasitic Neglected Tropical Diseases. Open
A series of thirty 1,2,3-triazolylsterols were prepared by a stereocontrolled synthesis and inspired by azasterols with proven antiparasitic activity. Ten of these compounds constitute chimeras/hybrids of AZA and 1,2,3-triazolyl azasterols…
View article: Preclinical Studies in Anti-Trypanosomatidae Drug Development
Preclinical Studies in Anti-Trypanosomatidae Drug Development Open
The trypanosomatid parasites Trypanosoma brucei, Trypanosoma cruzi and Leishmania are the causative agents of human African trypanosomiasis, Chagas Disease and Leishmaniasis, respectively. These infections primarily affect poor, rural comm…
View article: Unraveling the antitrypanosomal mechanism of benznidazole and related 2‐nitroimidazoles: From prodrug activation to DNA damage
Unraveling the antitrypanosomal mechanism of benznidazole and related 2‐nitroimidazoles: From prodrug activation to DNA damage Open
Nitroheterocycles represent an important class of compound used to treat trypanosomiasis. They often function as prodrugs and can undergo type I nitroreductase (NTR1)‐mediated activation before promoting their antiparasitic activities alth…
View article: CCDC 2039709: Experimental Crystal Structure Determination
CCDC 2039709: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2039710: Experimental Crystal Structure Determination
CCDC 2039710: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Evaluation of trypanocidal properties of ferrocenyl and cyrhetrenyl N-acylhydrazones with pendant 5-nitrofuryl group
Evaluation of trypanocidal properties of ferrocenyl and cyrhetrenyl N-acylhydrazones with pendant 5-nitrofuryl group Open
View article: Challenges in Chagas Disease Drug Development
Challenges in Chagas Disease Drug Development Open
The protozoan parasite Trypanosoma cruzi causes Chagas disease, an important public health problem throughout Latin America. Current therapeutic options are characterised by limited efficacy, long treatment regimens and frequent toxic side…
View article: CCDC 1972618: Experimental Crystal Structure Determination
CCDC 1972618: Experimental Crystal Structure Determination Open
View article: CCDC 1972620: Experimental Crystal Structure Determination
CCDC 1972620: Experimental Crystal Structure Determination Open
View article: Deciphering the interstrand crosslink DNA repair network expressed by<i>Trypanosoma brucei</i>
Deciphering the interstrand crosslink DNA repair network expressed by<i>Trypanosoma brucei</i> Open
Interstrand crosslinks (ICLs) represent a highly toxic form of DNA damage that can block essential biological processes including DNA replication and transcription. To combat their deleterious effects all eukaryotes have developed cell cyc…
View article: Cyrhetrenylaniline and new organometallic phenylimines derived from 4- and 5-nitrothiophene: Synthesis, characterization, X-Ray structures, electrochemistry and in vitro anti-T. brucei activity
Cyrhetrenylaniline and new organometallic phenylimines derived from 4- and 5-nitrothiophene: Synthesis, characterization, X-Ray structures, electrochemistry and in vitro anti-T. brucei activity Open
View article: CCDC 1586088: Experimental Crystal Structure Determination
CCDC 1586088: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1586087: Experimental Crystal Structure Determination
CCDC 1586087: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1586086: Experimental Crystal Structure Determination
CCDC 1586086: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Functional characterisation of the methionine sulfoxide reductase repertoire in Trypanosoma brucei
Functional characterisation of the methionine sulfoxide reductase repertoire in Trypanosoma brucei Open
View article: Distinct activation mechanisms trigger the trypanocidal activity of DNA damaging prodrugs
Distinct activation mechanisms trigger the trypanocidal activity of DNA damaging prodrugs Open
Summary Quinone‐based compounds have been exploited to treat infectious diseases and cancer, with such chemicals often functioning as inhibitors of key metabolic pathways or as prodrugs. Here, we screened an aziridinyl 1,4‐benzoquinone (AB…
View article: Identification of Specific Inhibitors of Trypanosoma cruzi Malic Enzyme Isoforms by Target-Based HTS
Identification of Specific Inhibitors of Trypanosoma cruzi Malic Enzyme Isoforms by Target-Based HTS Open
Trypanosoma cruzi is the causative agent of Chagas disease. The lack of an efficient and safe treatment supports the research into novel metabolic targets, with the malic enzyme (ME) representing one such potential candidate. T. …
View article: Characterisation of the fumarate hydratase repertoire in Trypanosoma cruzi
Characterisation of the fumarate hydratase repertoire in Trypanosoma cruzi Open
View article: Nitrotriazole-based acetamides and propanamides with broad spectrum antitrypanosomal activity
Nitrotriazole-based acetamides and propanamides with broad spectrum antitrypanosomal activity Open
View article: Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds
Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds Open
View article: Evaluating 5-Nitrothiazoles as Trypanocidal Agents
Evaluating 5-Nitrothiazoles as Trypanocidal Agents Open
The growth-inhibitory properties of a 5-nitrothiazole series were evaluated against Trypanosoma brucei . A subset of related compounds displayed the greatest potency toward the parasite while exhibiting little cytotoxic effect on mammalian…
View article: 3-Nitrotriazole-based piperazides as potent antitrypanosomal agents
3-Nitrotriazole-based piperazides as potent antitrypanosomal agents Open
View article: Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation
Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation Open
View article: The Trypanosoma cruzi Vitamin C Dependent Peroxidase Confers Protection against Oxidative Stress but Is Not a Determinant of Virulence
The Trypanosoma cruzi Vitamin C Dependent Peroxidase Confers Protection against Oxidative Stress but Is Not a Determinant of Virulence Open
TcAPx is not essential for parasite viability within the mammalian host, does not have a significant role in establishment or maintenance of chronic infections, and should therefore not be considered a priority for drug design.
View article: Unravelling the role of <scp>SNM</scp>1 in the <scp>DNA</scp> repair system of <scp><i>T</i></scp><i>rypanosoma brucei</i>
Unravelling the role of <span>SNM</span>1 in the <span>DNA</span> repair system of <span><i>T</i></span><i>rypanosoma brucei</i> Open
Summary All living cells are subject to agents that promote DNA damage. A particularly lethal lesion are interstrand cross‐links ( ICL ), a property exploited by several anti‐cancer chemotherapies. In yeast and humans, an enzyme that plays…
View article: Novel 3-Nitrotriazole-Based Amides and Carbinols as Bifunctional Antichagasic Agents
Novel 3-Nitrotriazole-Based Amides and Carbinols as Bifunctional Antichagasic Agents Open
3-Nitro-1H-1,2,4-triazole-based amides with a linear, rigid core and 3-nitrotriazole-based fluconazole analogues were synthesized as dual functioning antitrypanosomal agents. Such compounds are excellent substrates for type I nitroreductas…