A. Konradi

发表

Porphyromonas gingivalis in Alzheimer’s disease brains: Evidence for disease causation and treatment with small-molecule inhibitors

D. Raha, M. Dragunow, E. Reynolds, 2019, Science Advances.

Intermolecular Pinacol Cross Coupling of Electronically Similar Aldehydes. An Efficient and Stereoselective Synthesis of 1,2-Diols Employing a Practical Vanadium(II) Reagent.

A. Konradi, J. Freudenberger, S. F. Pedersen, 1990 .

Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents.

H. Sham, N. Yao, T. Yednock, 2010, Bioorganic & medicinal chemistry letters.

Arylsulfonamide pyrimidines as VLA-4 antagonists.

L. Mutter, T. Yednock, F. Bard, 2013, Bioorganic & medicinal chemistry letters.

Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.

R. Neitz, H. Sham, N. Yao, 2011, Bioorganic & medicinal chemistry letters.

PEG conjugates of potent α4 integrin inhibitors, maintaining sustained levels and bioactivity in vivo, following subcutaneous administration.

C. Vandevert, T. Yednock, D. Quincy, 2013, Bioorganic & medicinal chemistry letters.

Highly selective c-Jun N-terminal kinase (JNK) 3 inhibitors with in vitro CNS-like pharmacokinetic properties II. Central core replacement.

R. Neitz, H. Sham, T. Yednock, 2011, Bioorganic & medicinal chemistry letters.

Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.

G. Tóth, R. Neitz, H. Sham, 2010, Bioorganic & medicinal chemistry letters.

The identification and optimization of orally efficacious, small molecule VLA-4 antagonists.

D. Huryn, S. Ashwell, T. Yednock, 2004, Current topics in medicinal chemistry.

Hippo pathway regulation by phosphatidylinositol transfer protein and phosphoinositides

W. Gerwick, B. Cravatt, K. Guan, 2022, Nature Chemical Biology.

Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.

G. Tóth, H. Sham, N. Yao, 2011, Bioorganic & medicinal chemistry letters.

Optimization of LpxC Inhibitors for Antibacterial Activity and Cardiovascular Safety.

F. Cohen, A. Jubb, Z. Wang, 2019 .

Optimization of LpxC Inhibitors for Antibacterial Activity and Cardiovascular Safety

F. Cohen, A. Jubb, K. Krause, 2019, ChemMedChem.

Orally available and efficacious α4β1/α4β7 integrin inhibitors.

Zhenmei Liao, L. Mutter, G. Shopp, 2013, Bioorganic & medicinal chemistry letters.

Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors.

H. Sham, T. Yednock, M. Bova, 2009, Bioorganic & medicinal chemistry letters.

Intermolecular pinacol cross coupling of aryl aldehydes or their dimethyl acetals with non-aryl aldehydes

P. Takahara, A. Konradi, J. Freudenberger, 1989 .

Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.

R. Motter, D. Kholodenko, H. Sham, 2010, Bioorganic & medicinal chemistry letters.

A facile synthesis of multigram quantity of ethyl 3-ethylmorpholine-3-carboxylate

H. Sham, L. Latimer, D. Quincy, 2011 .

Pinacol Cross Coupling of 2-[N-(Alkoxycarbonyl)amino] Aldehydes and Aliphatic Aldehydes by [V2Cl3(THF)6]2[Zn2Cl6]. Synthesis of syn,syn-3-[N-(Alkoxycarbonyl)amino] 1,2-Diols

S. Kemp, A. Konradi, S. F. Pedersen, 1994 .

Intermolecular pinacol cross coupling of electronically similar aldehydes. An efficient and stereoselective synthesis of 1,2-diols employing a practical vanadium(II) reagent

A. Konradi, J. Freudenberger, S. F. Pedersen, 1989 .

Stereoselective synthesis of 3-amino 1,2-diols via intermolecular pinacol cross-coupling of .alpha.-[(alkoxycarbonyl)amino] aldehydes with aliphatic aldehydes. Short asymmetric syntheses of two 2,3,6-trideoxy-3-amino sugars

A. Konradi, S. F. Pedersen, 1990 .

Pinacol homocoupling of (S)-2-[N-(benzyloxycarbonyl)amino] aldehydes by [V2Cl3(THF)6]2[Zn2Cl6]. Synthesis of C2-symmetric (1S,2R,3R,4S)-1,4-diamino 2,3-diols

A. Konradi, S. F. Pedersen, 1992 .

Small Molecule Inhibitors of TEAD Auto-palmitoylation Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma

K. Guan, T. Tang, L. Post, 2021, Molecular Cancer Therapeutics.

Selective and Brain‐Permeable Polo‐like Kinase‐2 (Plk‐2) Inhibitors That Reduce α‐Synuclein Phosphorylation in Rat Brain

Kent Fitzgerald, Paul Beroza, Lee Latimer, 2013, ChemMedChem.

Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors.

P. Beroza, R. Motter, R. Neitz, 2013, Bioorganic & medicinal chemistry letters.

Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates.

Paul Beroza, Zhao Ren, Dean R Artis, 2013, Bioorganic & medicinal chemistry letters.

Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease

R. Motter, D. Kholodenko, R. Barbour, 2010, Alzheimer's Research & Therapy.

Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.

John-Michael Sauer, Zhao Ren, Dean R Artis, 2011, Bioorganic & medicinal chemistry letters.

Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007): metabolically stable γ-secretase Inhibitor

R. Motter, D. Kholodenko, H. Sham, 2013, Journal of medicinal chemistry.

Transcriptional repression of estrogen receptor alpha by YAP reveals the Hippo pathway as therapeutic target for ER+ breast cancer

Xiang-Dong Fu, K. Guan, T. Tang, 2022, Nature communications.

Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.

H. Sham, L. Latimer, M. Bova, 2013, Bioorganic & medicinal chemistry letters.

Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region.

G. Tóth, H. Sham, N. Yao, 2010, Bioorganic & medicinal chemistry letters.

Transcriptional repression of estrogen receptor alpha by YAP reveals the Hippo pathway as therapeutic target for ER+ breast cancer

Xiang-Dong Fu, K. Guan, T. Tang, 2022, Nature Communications.

Discovery of sulfonamide-pyrazole gamma-secretase inhibitors.

H. Sham, J. Sauer, P. Keim, 2010, Bioorganic & medicinal chemistry letters.

Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: prime side chromane-containing inhibitors.

R. Neitz, M. Adler, H. Sham, 2012, Bioorganic & medicinal chemistry letters.

Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors.

H. Sham, M. Bova, J. Sauer, 2010, Bioorganic & Medicinal Chemistry Letters.

Design, synthesis and structure-activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent γ-secretase inhibitors.

H. Sham, M. Bova, J. Sauer, 2011, Bioorganic & medicinal chemistry letters.

Amino-caprolactam γ-secretase inhibitors showing potential for the treatment of Alzheimer's disease.

M. Bova, J. Sauer, G. Basi, 2011, Bioorganic & medicinal chemistry letters.

Discovery of a potent, orally bioavailable pyrimidine VLA-4 antagonist effective in a sheep asthma model.

W. Dunn, L. Mutter, C. Vandevert, 2011, Bioorganic & Medicinal Chemistry Letters.

Synthesis, characterization and evaluation of pro-drugs of VLA-4 antagonists.

D. Huryn, S. Ashwell, A. Konradi, 2004, Bioorganic & medicinal chemistry letters.

N-Bridged bicyclic sulfonamides as inhibitors of gamma-secretase.

H. Sham, M. Bova, J. Sauer, 2009, Bioorganic & medicinal chemistry letters.

R. Motter, D. Kholodenko, H. Sham, 2013, Journal of medicinal chemistry.

Correction: Label Free Fragment Screening Using Surface Plasmon Resonance as a Tool for Fragment Finding – Analyzing Parkin, a Difficult CNS Target

P. Beroza, K. Regnström, Jiangli Yan, 2013, PLoS ONE.

Label Free Fragment Screening Using Surface Plasmon Resonance as a Tool for Fragment Finding – Analyzing Parkin, a Difficult CNS Target

P. Beroza, K. Regnström, Jiangli Yan, 2013, PloS one.

Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents.

John-Michael Sauer, Gergely Toth, G. Tóth, 2009, Bioorganic & medicinal chemistry letters.

Selective and Brain‐Permeable Polo‐like Kinase‐2 (Plk‐2) Inhibitors That Reduce α‐Synuclein Phosphorylation in Rat Brain

P. Beroza, R. Motter, R. Neitz, 2013, ChemMedChem.