H. Pauls

发表

Spiro-naphthyridinone piperidines as inhibitors of S. aureus and E. coli enoyl-ACP reductase (FabI).

P. Sampson, N. Kaplan, D. Awrey, 2009, Bioorganic & medicinal chemistry letters.

2,3,4,5-Tetrahydro-1H-pyrido[2,3-b and e][1,4]diazepines as inhibitors of the bacterial enoyl ACP reductase, FabI.

David D. Manning, P. Sampson, N. Kaplan, 2009, Bioorganic & medicinal chemistry letters.

Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent.

Narendra Kumar Patel, Y. Liu, T. Mak, 2016, ACS medicinal chemistry letters.

The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents.

Narendra Kumar Patel, Y. Liu, T. Mak, 2015, Journal of medicinal chemistry.

Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides.

Narendra Kumar Patel, T. Mak, N. Chirgadze, 2014, Bioorganic & medicinal chemistry.

The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents.

Narendra Kumar Patel, T. Mak, N. Chirgadze, 2015 .

Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency.

C. Dunwiddie, D. Cheney, A. Spada, 2002, Bioorganic & medicinal chemistry letters.

Characterization of the bisphosphonate recognition site on hydroxyapatite using radioligand binding techniques with [14C]citric acid

D. Cheney, M. Jarvis, C. Burns, 1993, Calcified Tissue International.

New inhibitors of cysteine proteinases. Peptidyl acyloxymethyl ketones and the quiescent nucleofuge strategy

A. Krantz, L. Copp, S. Heard, 1988 .

Novel pyrazinone inhibitors of mast cell tryptase: synthesis and SAR evaluation.

M. Mathieu, C. Hopkins, S. Jackson, 2004, Bioorganic & medicinal chemistry letters.

The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents.

Y. Liu, T. Mak, P. Sampson, 2013, Journal of medicinal chemistry.

The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents.

Narendra Kumar Patel, Y. Liu, T. Mak, 2015, Journal of medicinal chemistry.

Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase.

M. Mathieu, C. Hopkins, S. Kaye, 2005, Bioorganic & medicinal chemistry letters.

Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.

A. Spada, D. Colussi, Y. Gong, 2000, Bioorganic & medicinal chemistry letters.

Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand.

Robert Leadley, Guyan Liang, R. Bentley, 2003, Journal of medicinal chemistry.

Aminoisoquinolines: design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA.

C. Dunwiddie, D. Cheney, R. Bentley, 1999, Bioorganic & medicinal chemistry letters.

Crystal structures of human factor Xa complexed with potent inhibitors.

A. Spada, W. R. Ewing, V. Mikol, 2000, Journal of medicinal chemistry.

Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.

R. Bentley, A. Spada, C. Ly, 1999, Bioorganic & medicinal chemistry letters.

Dimerization of β-tryptase inhibitors, does it work for both basic and neutral P1 groups?

I. Morize, Xin Chen, G. Liang, 2012, Bioorganic & medicinal chemistry letters.

Solid-phase parallel synthesis of azarene pyrrolidinones as factor Xa inhibitors.

J. Salvino, Y. M. Choi-Sledeski, Y. Gong, 2000, Bioorganic & medicinal chemistry letters.

The Design of Competitive, Small-molecule Inhibitors of Coagulation Factor Xa

W. R. Ewing, Y. M. Choi-Sledeski, H. Pauls, 2001 .

Structure based design of 4-(3-aminomethylphenyl)piperidinyl-1-amides: novel, potent, selective, and orally bioavailable inhibitors of βII tryptase

S. Rebello, D. Engers, A. Dupuy, 2005 .

A short, efficient route to a protected daunosamine from L-rhamnose

H. Pauls, B. Fraser-Reid, 1984 .

A novel synthesis of methyl .alpha.-L-garosaminide which illustrates a stereocontrolled approach to the cis-hydroxyamino moiety of amino sugars

H. Pauls, B. Fraser-Reid, 1980 .

2-(Peptidamido)-cyclobutanones: A novel strategy for the inhibition of serine elastases

L. Reid, H. Pauls, B. Cheng, 1992 .

An efficient synthesis of ristosamine utilizing the allylic hydroxyl of a hex-2-enopyranoside

H. Pauls, B. Fraser-Reid, 1983 .

Stereocontrolled routes to cis-hydroxyamino sugars. Part VI. A synthesis of garosamine

H. Pauls, B. Fraser-Reid, 1984 .

Chiral building blocks for amphotericin B

M. Georges, S. Jarosz, H. Pauls, 1986 .

A NOVEL SYNTHESIS OF METHYL α-L-GAROSAMINIDE WHICH ILLUSTRATES A STEREOCONTROLLED APPROACH TO THE CIS-HYDROXYAMINO MOIETY OF AMINO SUGARS

H. Pauls, B. Fraser-Reid, 1980 .

Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK.

Y. Liu, T. Mak, O. Plotnikova, 2016, Bioorganic & medicinal chemistry letters.

The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents.

Narendra Kumar Patel, Y. Liu, T. Mak, 2015, Journal of medicinal chemistry.

Molecular structures of human factor Xa complexed with ketopiperazine inhibitors: preference for a neutral group in the S1 pocket.

Sébastien Maignan, William R Ewing, A. Spada, 2003, Journal of medicinal chemistry.

Design and optimization of (3-aryl-1H-indazol-6-yl)spiro[cyclopropane-1,3'-indolin]-2'-ones as potent PLK4 inhibitors with oral antitumor efficacy.

Narendra Kumar Patel, T. Mak, P. Sampson, 2016, Bioorganic & medicinal chemistry letters.

Stereocontrolled routes to cis-hydroxyamino sugars, Part VII: Synthesis of daunosamine and ristosamine.

H. Pauls, B. Fraser-Reid, 1986, Carbohydrate research.

RPR120844, a Novel, Specific Inhibitor of Coagulation Factor Xa Inhibits Venous Thrombosis in the Rabbit

C. Dunwiddie, R. Bentley, A. Spada, 1999, Thrombosis and Haemostasis.

Irreversible inhibition of transglutaminases by sulfonium methylketones: optimization of specificity and potency with omega-aminoacyl spacers.

A. Krantz, D. Pliura, H. Pauls, 1992, Journal of enzyme inhibition.

Mode of Action, In Vitro Activity, and In Vivo Efficacy of AFN-1252, a Selective Antistaphylococcal FabI Inhibitor

Vladimir Romanov, Molly B. Schmid, N. Kaplan, 2012, Antimicrobial Agents and Chemotherapy.

In vitro activity (MICs and rate of kill) of AFN-1252, a novel FabI inhibitor, in the presence of serum and in combination with other antibiotics

N. Kaplan, D. Awrey, J. Yethon, 2013, Journal of chemotherapy.

A Convenient Synthesis of Heteroaryl Benzoic Acids via Suzuki Reaction

H. Pauls, Y. Gong, 2000 .

Structure-based library design and the discovery of a potent and selective mast cell β-tryptase inhibitor as an oral therapeutic agent.

I. Morize, M. Mathieu, Xin Chen, 2012, Bioorganic & medicinal chemistry letters.

Carbon-13 NMR characterization of the papain adduct formed by peptidyl acyloxy-, aryloxy-, and chloromethyl ketone irreversible inhibitors

A. Krantz, Roger A. Smith, H. Pauls, 1992 .

Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity.

Daniel L Cheney, C. Dunwiddie, D. Cheney, 2002, Bioorganic & medicinal chemistry letters.

The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent.

Narendra Kumar Patel, Y. Liu, T. Mak, 2015, Journal of medicinal chemistry.

Structure based design of 4-(3-aminomethylphenyl)piperidinyl-1-amides: novel, potent, selective, and orally bioavailable inhibitors of betaII tryptase.

S. Rebello, D. Engers, A. Dupuy, 2005, Bioorganic & medicinal chemistry.