Rui Moreira
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View article: Π-Π stacking stabilized polymeric micelles for hydrophobic drug delivery in the treatment of leishmaniasis
Π-Π stacking stabilized polymeric micelles for hydrophobic drug delivery in the treatment of leishmaniasis Open
Current control strategies for leishmaniases - a group of diseases caused by protozoan parasites of the genus Leishmania - rely on chemotherapy, which is often associated with significant drawbacks, including severe side effects and limite…
View article: When the lights went out: impacts of the April 2025 Iberian blackout on the Portuguese National Health Service sovereignty - a reflection on national defence, health sovereignty, risk, and infrastructural dependency
When the lights went out: impacts of the April 2025 Iberian blackout on the Portuguese National Health Service sovereignty - a reflection on national defence, health sovereignty, risk, and infrastructural dependency Open
The April 2025 blackout in the Iberian Peninsula severely disrupted The Portuguese National Health Service (NHS). It led to failures for over eight hours in power supply, digital systems, telecommunications, and inter-institutional coordin…
View article: Discovery and Validation of a Novel Class of Necroptosis Inhibitors Targeting RIPK1
Discovery and Validation of a Novel Class of Necroptosis Inhibitors Targeting RIPK1 Open
Necroptosis is a form of programmed cell death that, when dysregulated, is associated with cancer and inflammatory and neurodegenerative diseases. Here, starting from hits identified from a phenotypic high-throughput screen for inhibitors …
View article: Correction: Oliveira et al. Discovery of a Necroptosis Inhibitor Improving Dopaminergic Neuronal Loss after MPTP Exposure in Mice. Int. J. Mol. Sci. 2021, 22, 5289
Correction: Oliveira et al. Discovery of a Necroptosis Inhibitor Improving Dopaminergic Neuronal Loss after MPTP Exposure in Mice. Int. J. Mol. Sci. 2021, 22, 5289 Open
In the original publication [...]
View article: 32nd Annual GP2A Medicinal Chemistry Conference
32nd Annual GP2A Medicinal Chemistry Conference Open
The Group for the Promotion of Pharmaceutical Chemistry in Academia (GP2A) held its 32nd annual conference in August 2024 at the University of Coimbra, Portugal. There were 8 keynote presentations, 12 early career researcher oral presentat…
View article: Nitroaromatic-based triazene prodrugs to target the hypoxic microenvironment in glioblastoma
Nitroaromatic-based triazene prodrugs to target the hypoxic microenvironment in glioblastoma Open
Nitroaromatic-based triazene prodrugs elicited enhanced cytotoxicity and apoptosis in hypoxic LN-229 glioblastoma cells comparing to temozolomide, highlighting their therapeutic potential for glioblastoma multiforme.
View article: 4-Oxo-β-lactams as Covalent Inhibitors of the Mitochondrial Intramembrane Protease PARL
4-Oxo-β-lactams as Covalent Inhibitors of the Mitochondrial Intramembrane Protease PARL Open
Rhomboid proteases play a variety of physiological roles, but rhomboid protease inhibitors have been mostly developed for the E. coli model rhomboid GlpG. In this work, we screened different electrophilic scaffolds against the human mitoch…
View article: 4‐Oxo‐β‐Lactams as Novel Inhibitors for Rhomboid Proteases
4‐Oxo‐β‐Lactams as Novel Inhibitors for Rhomboid Proteases Open
Intramembrane serine proteases (rhomboid proteases) are involved in a variety of biological processes and are implicated in several diseases. Here, we report 4‐oxo‐β‐lactams as a novel scaffold for inhibition of rhomboids. We show that the…
View article: Front Cover: Facile Access to Structurally Diverse Antimalarial Indoles Using a One‐Pot A<sup>3</sup> Coupling and Domino Cyclization Approach (ChemMedChem 17/2023)
Front Cover: Facile Access to Structurally Diverse Antimalarial Indoles Using a One‐Pot A<sup>3</sup> Coupling and Domino Cyclization Approach (ChemMedChem 17/2023) Open
The Front Cover depicts a female Anopheles spp. mosquito, the vector of Plasmodium falciparum and perhaps the most iconic image associated with the fight against malaria, which inspects the structure of a new indole scaffold with promising…
View article: New Compound Combining an Integrase-Targeting Aptamer and a Small Interfering RNA Targeting the Trans-Activation Response/Poly A Region of HIV-1 Potently Suppresses HIV-1 Replication
New Compound Combining an Integrase-Targeting Aptamer and a Small Interfering RNA Targeting the Trans-Activation Response/Poly A Region of HIV-1 Potently Suppresses HIV-1 Replication Open
We have developed a novel aptamer-based siRNA delivery system for HIV therapy. Apsi510 was obtained by chemical conjugation of an anti-HIV integrase aptamer and an siRNA sequence targeting the HIV-1 TAR/poly A regions to a dendron [2-((4-(…
View article: Facile Access to Structurally Diverse Antimalarial Indoles Using a One‐Pot A<sup>3</sup> Coupling and Domino Cyclization Approach
Facile Access to Structurally Diverse Antimalarial Indoles Using a One‐Pot A<sup>3</sup> Coupling and Domino Cyclization Approach Open
A multistep and diversity‐oriented synthetic route aiming at the A 3 coupling/domino cyclization of o ‐ethynyl anilines, aldehydes and s ‐amines is described. The preparation of the corresponding precursors included a series of transformat…
View article: Spontaneous retroperitoneal biloma in a patient with choledocholithiasis: Presentation of case
Spontaneous retroperitoneal biloma in a patient with choledocholithiasis: Presentation of case Open
Biloma should be considered in the differential diagnosis of a patient presenting with right upper quadrant or epigastric pain and an intra-abdominal collection on imaging. Efforts should be made in order to offer a prompt diagnosis and tr…
View article: A Review of the Development of Multitarget Molecules against HIV-TB Coinfection Pathogens
A Review of the Development of Multitarget Molecules against HIV-TB Coinfection Pathogens Open
The human immunodeficiency virus (HIV) produces the pathologic basis of acquired immunodeficiency syndrome (AIDS). An increase in the viral load in the body leads to a decline in the number of T lymphocytes, compromising the patient’s immu…
View article: Polysulfone Membranes Doped with Human Neutrophil Elastase Inhibitors: Assessment of Bioactivity and Biocompatibility
Polysulfone Membranes Doped with Human Neutrophil Elastase Inhibitors: Assessment of Bioactivity and Biocompatibility Open
The use of polysulfone (PSU) hemodialysis (HD) membranes modified with bioactive compounds has gained relevance in chronic kidney disease (CKD) management. Compounds based on the 4-oxo-β-lactam scaffold have outstanding inhibitory ability …
View article: The Facets of Diversity: The EFMC Perspective**
The Facets of Diversity: The EFMC Perspective** Open
Diversity in science refers to cultivating talent, while promoting full inclusion across the community. In medicinal chemistry and chemical biology, it enhances creativity and encourages contributions from multiple perspectives, leading to…
View article: Chemoproteomics‐Enabled Identification of 4‐Oxo‐β‐Lactams as Inhibitors of Dipeptidyl Peptidases 8 and 9
Chemoproteomics‐Enabled Identification of 4‐Oxo‐β‐Lactams as Inhibitors of Dipeptidyl Peptidases 8 and 9 Open
Dipeptidyl peptidases 8 and 9 (DPP8/9) have gathered interest as drug targets due to their important roles in biological processes like immunity and tumorigenesis. Elucidation of their distinct individual functions remains an ongoing task …
View article: Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable, and Blood–Brain Barrier Penetrant PROTAC Degrader of Leucine-Rich Repeat Kinase 2
Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable, and Blood–Brain Barrier Penetrant PROTAC Degrader of Leucine-Rich Repeat Kinase 2 Open
Leucine-rich repeat kinase 2 (LRRK2) is one of the most promising targets for Parkinson's disease. LRRK2-targeting strategies have primarily focused on type 1 kinase inhibitors, which, however, have limitations as the inhibited protein can…
View article: Harnessing Protein-Ligand Interaction Fingerprints to Predict New Scaffolds of RIPK1 Inhibitors
Harnessing Protein-Ligand Interaction Fingerprints to Predict New Scaffolds of RIPK1 Inhibitors Open
Necroptosis has emerged as an exciting target in oncological, inflammatory, neurodegenerative, and autoimmune diseases, in addition to acute ischemic injuries. It is known to play a role in innate immune response, as well as in antiviral c…
View article: Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable and Blood Brain Barrier Penetrant Prote-olysis Targeting Chimera Degrader of Leucine Rich Repeat Kinase 2
Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable and Blood Brain Barrier Penetrant Prote-olysis Targeting Chimera Degrader of Leucine Rich Repeat Kinase 2 Open
Leucine Rich Repeat Kinase 2 (LRRK2) is one of the most promising targets for Parkinson’s Disease. LRRK2 targeting strategies have primarily focused on Type 1 kinase inhibitors, which however have limitations as the inhibited protein can i…
View article: Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Oral bioavailable and Blood Brain Barrier Penetrant PROTAC Degrader of Leucine Rich Repeat Kinase 2 (LRRK2)
Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Oral bioavailable and Blood Brain Barrier Penetrant PROTAC Degrader of Leucine Rich Repeat Kinase 2 (LRRK2) Open
Leucine Rich Repeat Kinase 2 (LRRK2) is one of the most promising targets for Parkinson’s Disease. LRRK2 targeting strategies have primarily focused on Type 1 kinase inhibitors, which however have limitations as the inhibited pro-tein can …
View article: MO752: Doping Polysulfone Dialysis Membranes with Human Neutrophil Elastase Inhibitors—A Proof-of-Concept Study
MO752: Doping Polysulfone Dialysis Membranes with Human Neutrophil Elastase Inhibitors—A Proof-of-Concept Study Open
BACKGROUND AND AIMS The recurrent contact of blood with the haemodialysis (HD) membrane during the treatment procedure, triggers neutrophil activation, leading to an increase of blood levels of neutrophil elastase that contributes to the c…
View article: Tandem Thio‐Michael Addition/Remote Lactone Activation of 5‐Hydroxymethylfurfural‐Derived δ‐Lactone‐Fused Cyclopentenones
Tandem Thio‐Michael Addition/Remote Lactone Activation of 5‐Hydroxymethylfurfural‐Derived δ‐Lactone‐Fused Cyclopentenones Open
The creation of structurally diverse chemical entities from fairly simple biorefinery products remains a challenge. In this work 5‐hydroxymethylfurfural (HMF) was identified as a key synthon for preparing highly complex cyclopentenones (CP…
View article: Indole-Containing Pyrazino[2,1-<i>b</i>]quinazoline-3,6-diones Active against <i>Plasmodium</i> and Trypanosomatids
Indole-Containing Pyrazino[2,1-<i>b</i>]quinazoline-3,6-diones Active against <i>Plasmodium</i> and Trypanosomatids Open
Malaria, leishmaniasis, and sleeping sickness are potentially fatal diseases that represent a real health risk for more than 3,5 billion people. New antiparasitic compounds are urgent leading to a constant search for novel scaffolds. Herei…
View article: Discovery of a Necroptosis Inhibitor Improving Dopaminergic Neuronal Loss after MPTP Exposure in Mice
Discovery of a Necroptosis Inhibitor Improving Dopaminergic Neuronal Loss after MPTP Exposure in Mice Open
Parkinson’s disease (PD) is the second most common neurodegenerative disorder, mainly characterized by motor deficits correlated with progressive dopaminergic neuronal loss in the substantia nigra pars compacta (SN). Necroptosis is a caspa…
View article: Biological Evaluation and Mechanistic Studies of Quinolin-(1 <i>H</i> )-Imines as a New Chemotype against Leishmaniasis
Biological Evaluation and Mechanistic Studies of Quinolin-(1 <i>H</i> )-Imines as a New Chemotype against Leishmaniasis Open
Leishmaniasis is one of the most challenging neglected tropical diseases and remains a global threat to public health. Currently available therapies for leishmaniases present significant drawbacks and are rendered increasingly inefficient …