Discovery of Raltegravir, a Potent, Selective Orally Bioavailable HIV-Integrase Inhibitor for the Treatment of HIV-AIDS Infection

Vincenzo Summa, Alessia Petrocchi, Fabio Bonelli, +20

Journal of Medicinal Chemistry

Antiviral DrugMedicinal ChemistryAntiviral Drug DevelopmentResistance Mutation (Virology)Biochemistry +14

Molecular Insights into Quorum Sensing in the Human Pathogen Pseudomonas aeruginosa from the Structure of the Virulence Regulator LasR Bound to Its Autoinducer

Matthew J. Bottomley, Ester Muraglia, Renzo Bazzo

Journal of Biological Chemistry

Crystal StructureSymmetrical DimerQuorum SensingNatural SciencesVirulence Factor +12

In Vitro Selection and Characterization of Hepatitis C Virus Serine Protease Variants Resistant to an Active-Site Peptide Inhibitor

Caterina Trozzi, Linda Bartholomew, Alessandra Ceccacci, +10

Journal of Virology

4,5-Dihydroxypyrimidine Carboxamides and <i>N</i>-Alkyl-5-hydroxypyrimidinone Carboxamides Are Potent, Selective HIV Integrase Inhibitors with Good Pharmacokinetic Profiles in Preclinical Species

Vincenzo Summa, Alessia Petrocchi, Victor G. Matassa, +7

Journal of Medicinal Chemistry

Bioorganic ChemistryPharmacotherapyAntiviral DrugMedicinal Chemistry4,5-Dihydroxypyrimidine Carboxamides +15

Tetrazole thioacetanilides: Potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant

Ester Muraglia, Olaf Kinzel, Ralph Laufer, +9

Bioorganic & Medicinal Chemistry Letters

MedicineNatural SciencesHuman RetrovirusAntiviral Drug DevelopmentMolecular Biology +10

Homolytic substitution reactions of electron-rich pentatomic heteroaromatics by electrophilic carbon-centered radicals. Synthesis of .alpha.-heteroarylacetic acids

Enrico Baciocchi, Ester Muraglia, G. SLEITER

The Journal of Organic Chemistry

EngineeringHeterocyclicBiochemistryNatural SciencesElectrosynthesis +12

A novel, inducible, eukaryotic gene expression system based on the quorum‐sensing transcription factor TraR

Petra Neddermann, Cesare Gargioli, Ester Muraglia, +4

EMBO Reports

Transcriptional RegulationNatural SciencesGene RegulationMolecular BiologyTranscription Factor Trar +6

Dihydroxypyrimidine-4-carboxamides as Novel Potent and Selective HIV Integrase Inhibitors

Paola Pace, Maria Emilia Di Francesco, Cristina Gardelli, +15

Journal of Medicinal Chemistry

Combinatorial ChemistryMedicinal ChemistryBioorganic ChemistryInteresting CompoundsBiochemistry +13

Discovery and Synthesis of HIV Integrase Inhibitors:  Development of Potent and Orally Bioavailable N-Methyl Pyrimidones

Cristina Gardelli, Emanuela Nizi, Ester Muraglia, +23

Journal of Medicinal Chemistry

Medicinal ChemistryInteresting CompoundsBiochemistryMedicineDrug Discovery +13

Identification of Novel, Selective, and Stable Inhibitors of Class II Histone Deacetylases. Validation Studies of the Inhibition of the Enzymatic Activity of HDAC4 by Small Molecules as a Novel Approach for Cancer Therapy

Jesus M. Ontoria, Sergio Altamura, Annalise Di Marco, +10

Journal of Medicinal Chemistry