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Concept

Pharmacologie

Publications associées (31)

Synthesis of diphenoxyadamantane alkylamines with pharmacological interest

Stewart Cole, Anthony Vocat

In this work, the synthesis and the pharmacological evaluation of diphenoxyadamantane alkylamines Ia-f and IIa-f is described. The new diphenoxy-substituted adamantanes share structural features present in trypanocidal and antitubercular agents. 1-Methylpi ...

PERGAMON-ELSEVIER SCIENCE LTD2019

Design and validation of bioorthogonal probes for cellular disease models

Pier Luca D'Alessandro

Well-validated chemical probes enable testing of biological hypotheses, investigation of target tractability and translatability to the clinical phase. Consequently, these important tool compounds play a key role in the drug discovery process. Moreover, th ...

EPFL2019

Efficient Kinetic Resolution of Sulfur-Stereogenic Sulfoximines by Exploiting (CpRhIII)-Rh-X-Catalyzed C-H Functionalization

Nicolai Cramer, Marcus Brauns

Chiral sulfoximines with stereogenic sulfur atoms are promising motifs in drug discovery. We report an efficient method to access chiral sulfoximines through a C-H functionalization based kinetic resolution. A rhodium(III) complex equipped with a chiral Cp ...

Wiley-VCH Verlag GmbH2019

Novel osmium(II)-cymene complexes containing curcumin and bisdemethoxycurcumin ligands

Paul Joseph Dyson, Lucinda Kate Batchelor

The first examples of (arene)Os(II) curcuminoid derivatives have been prepared and characterized. The neutral complexes [(p-cym)Os(curc)Cl] (1) and [( p-cym)Os(bdcurc)Cl] ( 2), together with the cationic derivatives [( p-cym)Os(curc)(PTA)][SO3CF3] (3) and ...

ROYAL SOC CHEMISTRY2019

From Patients to Platelets and Back Again: Pharmacological Approaches to Glycoprotein VI, a Thrilling Antithrombotic Target with Minor Bleeding Risks

Nikolaos Stergiopoulos, Augusto Martins Lima

Despite significant advances in the treatment of thrombogenic diseases, antiplatelet therapies are still associated with a high bleeding risk. Consequently, potential benefits of preventing thromboembolic events by pharmacological agents need to be balance ...

GEORG THIEME VERLAG KG2019

Neuropharmacology of the mesolimbic system and associated circuits on social hierarchies

Maria del Carmen Sandi Perez, Sriparna Ghosal

Most socially living species are organized hierarchically, primarily based on individual differences in social dominance. Dominant individuals typically gain privileged access to important resources, such as food, mating partners and territories, whereas s ...

2019

Synthesis, biology, computational studies and in vitro controlled release of new isoniazid-based adamantane derivatives

Stewart Cole, Anthony Vocat

Aim: There is a necessity for new drugs to be more efficient than today's standard due to the emergence of drug-resistant strains of Mycobacterium tuberculosis (Mtb) Results/methodology: 12 new isoniazid-based adamantane derivatives were synthesized and te ...

FUTURE SCI LTD2019

Inhibitor-conjugated harmonic nanoparticles targeting fibroblast activation protein

Sandrine Gerber, Raphaël Jovita De Matos, Jérémy Vuilleumier

The recent progress in the engineering of nanosized inorganic materials presenting tailored physical properties and reactive surface for post-functionalization has opened promising avenues for the use of nanoparticles (NPs) in diagnosis and therapeutic int ...

2019

Conservative management of retinoblastoma: Challenging orthodoxy without compromising the state of metastatic grace. "Alive, with good vision and no comorbidity"

Paul Joseph Dyson

Retinoblastoma is lethal by metastasis if left untreated, so the primary goal of therapy is to preserve life, with ocular survival, visual preservation and quality of life as secondary aims. Historically, enucleation was the first successful therapeutic ap ...

PERGAMON-ELSEVIER SCIENCE LTD2019

A reduced form of nicotinamide riboside defines a new path for NAD(+) biosynthesis and acts as an orally bioavailable NAD(+) precursor

Richardus Houtkooper, Carlos Canto Alvarez

Objective: A decay in intracellular NAD(+) levels is one of the hallmarks of physiological decline in normal tissue functions. Accordingly, dietary supplementation with NAD(+) precursors can prevent, alleviate, or even reverse multiple metabolic complicati ...

2019

New Binding Sites, New Opportunities for GPCR Drug Discovery

Horst Arthur Vogel, Yen-Huan Li, Shuguang Yuan, Yifan Li, Thamani Dahoun

Many central biological events rely on protein-ligand interactions. The identification and characterization of protein-binding sites for ligands are crucial for the understanding of functions of both endogenous ligands and synthetic drug molecules. G prote ...

ELSEVIER SCIENCE LONDON2019