Application of Fragment-Based Lead Generation to the Discovery of Novel, Cyclic Amidine β-Secretase Inhibitors with Nanomolar Potency, Cellular Activity, and High Ligand Efficiency

Philip D. Edwards, Jeffrey S. Albert, Mark Sylvester, +19

Journal of Medicinal Chemistry

Discovery of a Novel Warhead against β-Secretase through Fragment-Based Lead Generation

Stefan Geschwindner, Lise‐Lotte Olsson, Jeffrey S. Albert, +4

Journal of Medicinal Chemistry

Medicinal ChemistryDrug TargetFragment-based Lead GenerationFragment HitsBiochemistry +13

Linear Non-competitive Inhibition of Solubilized Human γ-Secretase by Pepstatin A Methylester, L685458, Sulfonamides, and Benzodiazepines

Gaochao Tian, Cynthia D. Sobotka‐Briner, John R. Zysk, +6

Journal of Biological Chemistry

Cerebral DepositionNeurochemical BiomarkersPeptide SciencePharmacotherapyAnalytical Ultracentrifugation +20

Design, synthesis, and kinetic evaluation of a unique class of elastase inhibitors, the peptidyl .alpha.-ketobenzoxazoles, and the x-ray crystal structure of the covalent complex between porcine pancreatic elastase and Ac-Ala-Pro-Val-2-benzoxazole

Philip D. Edwards, Edgar F. Meyer, J. Vijayalakshmi, +4

Journal of the American Chemical Society

Unique ClassInhibitory ActivityMedicinal ChemistryPharmaceutical ScienceElastase Inhibitors +13

Application of Fragment Screening by X-ray Crystallography to the Discovery of Aminopyridines as Inhibitors of β-Secretase

Miles Congreve, David Aharony, Jeffrey S. Albert, +11

Journal of Medicinal Chemistry

Conversion of Cystitis Glandularis to Adenocarcinoma

Philip D. Edwards, Raymond A. Hurm, Walter H. Jaeschke

The Journal of Urology

Urogenital RadiologyUrological ResearchSurgical OncologyUrologyTumoral Pathology +13

.alpha.-Amino carbanions via formamidines. Alkylation of pyrrolidines, piperidines, and related heterocycles

A. I. MEYERS, Philip D. Edwards, William F. Rieker, +1

Journal of the American Chemical Society

Altmetric Attention ScoreOrganic ChemistryChemistryHeterocycle ChemistryPharmaceutical Chemistry +14

.alpha.-Amino carbanions. Preparation, metalation, and alkylation of enamidines. Synthesis of piperidine and pyrrolidine natural products and homologation of carbonyl compounds

A. L. Meyers, Philip D. Edwards, T. R. Bailey, +1

The Journal of Organic Chemistry

Combinatorial ChemistryCarbonyl CompoundsNatural Product SynthesisEngineeringAltmetric Attention Score +11

Orally Active Trifluoromethyl Ketone Inhibitors of Human Leukocyte Elastase

Chris A. Veale, Peter R Bernstein, Claudia Bohnert, +22

Journal of Medicinal Chemistry

Medicinal ChemistryOral BioavailabilityPharmaceutical ScienceBiochemistryHuman Leukocyte Elastase +11

Peptidyl .alpha.-ketoheterocyclic inhibitors of human neutrophil elastase. 2. Effect of varying the heterocyclic ring on in vitro potency

Philip D. Edwards, Donald J. Wolanin, Donald W. Andisik, +1

Journal of Medicinal Chemistry