A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase

Daria J. Hazuda, Neville J. Anthony, Robert Gomez, +30

Proceedings of the National Academy of Sciences

Hiv-1 IntegraseImmunologyCell CulturePharmacotherapyAntiviral Drug +15

Design and Synthesis of 8-Hydroxy-[1,6]Naphthyridines as Novel Inhibitors of HIV-1 Integrase in Vitro and in Infected Cells

Linghang Zhuang, John Wai, Mark W. Embrey, +17

Journal of Medicinal Chemistry

Hiv-1 IntegraseBiochemistryMedicineImmunologyAntiviral Drug Development +12

4-Aryl-2,4-dioxobutanoic Acid Inhibitors of HIV-1 Integrase and Viral Replication in Cells

John Wai, Melissa S. Egbertson, Linda S. Payne, +18

Journal of Medicinal Chemistry

Hiv-1 IntegraseViral ReplicationImmunologyAltmetric Attention ScoreCell Culture +15

Inhibition of HIV-1 Ribonuclease H by a Novel Diketo Acid, 4-[5-(Benzoylamino)thien-2-yl]-2,4-dioxobutanoic Acid

Cathryn A. Shaw-Reid, Vandna Munshi, Pia Graham, +10

Journal of Biological Chemistry

Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity

Jack D. Scott, Duane E. DeMong, Thomas J. Greshock, +42

Journal of Medicinal Chemistry

Drug TargetPharmacotherapyMedicinal ChemistryBrain Kinase ActivityLrrk2 Inhibitors +14

A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors

Thomas J. Tucker, Mark W. Embrey, Candice Alleyne, +27

Journal of Medicinal Chemistry

Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design

Candice Alleyne, Rupesh P. Amin, Bhavana Bhatt, +26

Journal of Medicinal Chemistry

A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells

Mark W. Embrey, John Wai, Timothy W. Funk, +19

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryHiv-1 IntegraseViral ReplicationMedicineImmunology +8

A potent and orally active HIV-1 integrase inhibitor

Melissa S. Egbertson, H. Moritz, Jeffrey Y. Melamed, +24

Bioorganic & Medicinal Chemistry Letters

MedicineImmunologyAntiviral Drug DevelopmentAntiviral TherapyAntiviral Drug +3

Discovery of 2-Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV-1 Integrase Strand Transfer Inhibitors

Izzat T. Raheem, Abbas M. Walji, Daniel J. Klein, +25

Journal of Medicinal Chemistry

Lead CompoundsPharmacotherapyAntiviral DrugChemical BiologyPharmaceutical Chemistry +17