Discovery and preclinical characterization of [18F]PI-2620, a next-generation tau PET tracer for the assessment of tau pathology in Alzheimer’s disease and other tauopathies

Heiko Kroth, Felix Oden, Jérôme Molette, +17

European Journal of Nuclear Medicine and Molecular Imaging

Development and Pharmacological Characterization of Selective Blockers of 2-Arachidonoyl Glycerol Degradation with Efficacy in Rodent Models of Multiple Sclerosis and Pain

Margherita Brindisi, Samuele Maramai, Sandra Gemma, +24

Journal of Medicinal Chemistry

NeuropeptidesPain MedicineCompound 4AMolecular PainPharmacotherapy +18

Mimicking the Intramolecular Hydrogen Bond: Synthesis, Biological Evaluation, and Molecular Modeling of Benzoxazines and Quinazolines as Potential Antimalarial Agents

Sandra Gemma, Caterina Camodeca, Margherita Brindisi, +21

Journal of Medicinal Chemistry

Combinatorial ChemistryBioorganic ChemistryAntiparasitic AgentMalariaOrganic Chemistry +15

Conformational Flexibility in the Peripheral Site of <i>Torpedo c</i><i>alifornica</i> Acetylcholinesterase Revealed by the Complex Structure with a Bifunctional Inhibitor

Jacques‐Philippe Colletier, Benoît Sanson, Florian Nachon, +4

Journal of the American Chemical Society

Protein ChemistryProteinlipid InteractionTorpedo Californica AcetylcholinesteraseProtein AssemblyBiochemistry +13

Discovery of Huperzine A−Tacrine Hybrids as Potent Inhibitors of Human Cholinesterases Targeting Their Midgorge Recognition Sites

Sandra Gemma, Emanuele Gabellieri, Paul B. Huleatt, +10

Journal of Medicinal Chemistry

BACE1 inhibitors: A head group scan on a series of amides

Thomas J. Woltering, Wolfgang Wostl, Hans Hilpert, +16

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryBioorganic ChemistryBiochemistryBace1 InhibitorsNatural Sciences +11

Synthesis of Dihydroplakortin, 6-<i>epi</i>-Dihydroplakortin, and Their C10-Desethyl Analogues

Sandra Gemma, Emanuele Gabellieri, Salvatore Sanna Coccone, +5

The Journal of Organic Chemistry

Medicinal ChemistryBiosynthesisBioorganic ChemistryStereogenic CentersBiochemistry +13

Synthetic studies toward 1,2-dioxanes as precursors of potential endoperoxide-containing antimalarials

Sandra Gemma, Francesc Martí, Emanuele Gabellieri, +3

Tetrahedron Letters

Potential Endoperoxide-containing AntimalarialsOrganic ChemistryChemistryHeterocycle ChemistryPharmacology +2

An Efficient Approach to Chiral C8/C9-Piperazino-Substituted 1,4-Benzodiazepin-2-ones as Peptidomimetic Scaffolds

Stefania Butini, Emanuele Gabellieri, Paul B. Huleatt, +9

The Journal of Organic Chemistry

<b>PI-2620</b> Lead Optimization Highlights the Importance of Off-Target Assays to Develop a PET Tracer for the Detection of Pathological Aggregated Tau in Alzheimer’s Disease and Other Tauopathies

Heiko Kroth, Felix Oden, Jérôme Molette, +12

Journal of Medicinal Chemistry