Brian J. Cox
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View article: Cell-Based Progression of Spiroindoline Phenotypic Hits Leads to the Identification of Compounds with Diverging Parasitological Profiles against the Human Malaria Parasite <i>Plasmodium falciparum</i>
Cell-Based Progression of Spiroindoline Phenotypic Hits Leads to the Identification of Compounds with Diverging Parasitological Profiles against the Human Malaria Parasite <i>Plasmodium falciparum</i> Open
In the search for novel chemotypes with high sp3 character and activity against the human malaria parasite Plasmodium falciparum, a spiroindoline series was identified from a phenotypic high-throughput screening campaign.…
View article: Cover Feature: The European Federation for Medicinal Chemistry and Chemical Biology (EFMC) Best Practice Initiative: Hit to Lead (ChemMedChem 8/2025)
Cover Feature: The European Federation for Medicinal Chemistry and Chemical Biology (EFMC) Best Practice Initiative: Hit to Lead (ChemMedChem 8/2025) Open
View article: The European Federation for Medicinal Chemistry and Chemical Biology (EFMC) Best Practice Initiative: Hit to Lead
The European Federation for Medicinal Chemistry and Chemical Biology (EFMC) Best Practice Initiative: Hit to Lead Open
The Hit to Lead (H2L) process is an integral part of contemporary drug discovery, encompassing the optimisation of validated Hit structures into Lead molecules. High quality leads build confidence, through activity and property profiles as…
View article: 1451. <i>Elizabethkingia spp</i>. Outbreak in a Ventilator-capable Skilled Nursing Facility, Chicago 2023
1451. <i>Elizabethkingia spp</i>. Outbreak in a Ventilator-capable Skilled Nursing Facility, Chicago 2023 Open
Background In July 2022, the Chicago Department of Public Health (CDPH) was notified of four residents with Elizabethkingia (Ek) infections at a ventilator-capable skilled nursing facility (vSNF A). The facility reviewed microbiology recor…
View article: CCDC 2190539: Experimental Crystal Structure Determination
CCDC 2190539: 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 2190540: Experimental Crystal Structure Determination
CCDC 2190540: 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: Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease
Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease Open
Mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel are established as the primary causative factor in the devastating lung disease cystic fibrosis (CF). More recently, cigarette smoke exposure has been …
View article: CCDC 2018589: Experimental Crystal Structure Determination
CCDC 2018589: Experimental Crystal Structure Determination Open
View article: CCDC 2032540: Experimental Crystal Structure Determination
CCDC 2032540: 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: Escaping from Flatland: Antimalarial Activity of sp<sup>3</sup>-Rich Bridged Pyrrolidine Derivatives
Escaping from Flatland: Antimalarial Activity of sp<sup>3</sup>-Rich Bridged Pyrrolidine Derivatives Open
We utilized synthetic photochemistry to generate novel sp3-rich scaffolds and report the design, synthesis, and biological testing of a diverse series of amides based on the 1-(amino-methyl)-2-benzyl-2-aza-bicyclo[2.1.1]hexane s…
View article: Circadian GLP-1 secretion in mice is dependent on the intestinal microbiome for maintenance of diurnal metabolic homeostasis
Circadian GLP-1 secretion in mice is dependent on the intestinal microbiome for maintenance of diurnal metabolic homeostasis Open
The incretin, glucagon-like peptide-1 (GLP-1), is secreted by the intestinal L-cell upon nutrient ingestion. GLP-1 also exhibits a circadian rhythm, with highest release at the onset of the feeding period. Similarly, microbial composition …
View article: Circadian GLP-1 secretion in mice is dependent on the intestinal microbiome for maintenance of diurnal metabolic homeostasis
Circadian GLP-1 secretion in mice is dependent on the intestinal microbiome for maintenance of diurnal metabolic homeostasis Open
The incretin, glucagon-like peptide-1 (GLP-1), is secreted by the intestinal L-cell upon nutrient ingestion. GLP-1 also exhibits a circadian rhythm, with highest release at the onset of the feeding period. Similarly, microbial composition …
View article: The European Federation for Medicinal Chemistry (EFMC) Best Practice Initiative: Validating Chemical Probes
The European Federation for Medicinal Chemistry (EFMC) Best Practice Initiative: Validating Chemical Probes Open
As part of an initiative aimed to share best practices in Medicinal Chemistry, the European Federation for Medicinal Chemistry (EFMC) is preparing a series of webinars and slide sets focused on the early phase of drug discovery. This educa…
View article: Escaping from Flatland: Substituted Bridged Pyrrolidine Fragments with Inherent Three-Dimensional Character
Escaping from Flatland: Substituted Bridged Pyrrolidine Fragments with Inherent Three-Dimensional Character Open
The pressure to deliver new medicines to the patient continues to grow along with increases in compound failure rate, thus putting the current R&D model at risk. Analysis has shown that increasing the three-dimensionality of potential drug…
View article: CCDC 1982731: Experimental Crystal Structure Determination
CCDC 1982731: 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: EMS Mutagenesis in Quinoa: Developing a Genetic Resource
EMS Mutagenesis in Quinoa: Developing a Genetic Resource Open
Chenopodium quinoa, a South American pseudocereal, has valuable agricultural traits such as salt tolerance and drought tolerance, and it has beneficial nutritional properties such as high protein content and a complete amino acid profile. …
View article: CCDC 1954037: Experimental Crystal Structure Determination
CCDC 1954037: Experimental Crystal Structure Determination Open
View article: CCDC 1954036: Experimental Crystal Structure Determination
CCDC 1954036: Experimental Crystal Structure Determination Open
View article: Shedding light on the use of Cu(<scp>ii</scp>)-salen complexes in the A<sup>3</sup> coupling reaction
Shedding light on the use of Cu(<span>ii</span>)-salen complexes in the A<sup>3</sup> coupling reaction Open
One air stable Cu(ii)-salen complex compound enables the generation of propargylamines. Mechanistic details, scope and limitations of this protocol are presented.
View article: Escaping from Flatland: [2 + 2] Photocycloaddition; Conformationally Constrained sp<sup>3</sup>-rich Scaffolds for Lead Generation
Escaping from Flatland: [2 + 2] Photocycloaddition; Conformationally Constrained sp<sup>3</sup>-rich Scaffolds for Lead Generation Open
Pressure on researchers to deliver new medicines to the patient continues to grow. Attrition rates in the research and development process present a significant challenge to the viability of the current model of drug discovery. Analysis sh…
View article: CCDC 1865126: Experimental Crystal Structure Determination
CCDC 1865126: 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: The Synthesis of Waltherione F and Its Analogues with Modifications at the 2‐ and 3‐Positions as Potential Antitrypanosomal Agents
The Synthesis of Waltherione F and Its Analogues with Modifications at the 2‐ and 3‐Positions as Potential Antitrypanosomal Agents Open
Chagas disease also know as American Trypanosomiasis (AT) is a tropical parasitic disease endemic in South America, is caused by Trypanosoma cruzi , which is transmitted by the blood‐sucking insect vectors called triatomine bugs. Quinoline…
View article: Cover Feature: Synthesis of a Novel Type of 2,3′‐BIMs via Platinum‐Catalysed Reaction of Indolylallenes with Indoles (Chem. Eur. J. 23/2018)
Cover Feature: Synthesis of a Novel Type of 2,3′‐BIMs via Platinum‐Catalysed Reaction of Indolylallenes with Indoles (Chem. Eur. J. 23/2018) Open
Organometallic synthesis is a powerful tool to make novel molecules with frameworks not encountered in natural products. In this context the platinum-catalysed reaction of indolylallenes with indole nucleophiles was discovered which gives …
View article: Synthesis of a Novel Type of 2,3′‐BIMs via Platinum‐Catalysed Reaction of Indolylallenes with Indoles
Synthesis of a Novel Type of 2,3′‐BIMs via Platinum‐Catalysed Reaction of Indolylallenes with Indoles Open
Optimisation, scope and mechanism of the platinum‐catalysed addition of indoles to indolylallenes is reported here to give 2,3′‐BIMs with a novel core structure very relevant for pharmaceutical industry. The reaction is modulated by the el…
View article: Correction to “Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP<sub>2</sub> Receptor Antagonist for Treatment of Asthma”
Correction to “Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP<sub>2</sub> Receptor Antagonist for Treatment of Asthma” Open
[This corrects the article DOI: 10.1021/acsmedchemlett.7b00157.].
View article: Identification of a Novel Allosteric Inhibitory Site on Tryptophan Hydroxylase 1 Enabling Unprecedented Selectivity Over all Related Hydroxylases
Identification of a Novel Allosteric Inhibitory Site on Tryptophan Hydroxylase 1 Enabling Unprecedented Selectivity Over all Related Hydroxylases Open
Pulmonary arterial hypertension (PAH) has demonstrated multi-serotonin receptor dependent pathologies, characterized by increased tone (5-HT1B receptor) and complex lesions (SERT, 5-HT1B, 5-HT2B receptors) of the pulmonary vasculature toge…
View article: Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP<sub>2</sub> Receptor Antagonist for Treatment of Asthma
Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP<sub>2</sub> Receptor Antagonist for Treatment of Asthma Open
Further optimization of an initial DP2 receptor antagonist clinical candidate NVP-QAV680 led to the discovery of a follow-up molecule 2-(2-methyl-1-(4-(methylsulfonyl)-2-(trifluoromethyl)benzyl)-1H-pyrrolo[2,3-b]py…