A. S. Nagle

Genomics Institute of the Novartis Research Foundation

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K. W. Jung

Berry & Associates (United States)

K. W. Jung

Kyung Woon Jung

University of Southern California

Arnab K. Chatterjee

Scripps Research Institute

Ralph Nicholas Salvatore

City University of New York

Elizabeth A. Winzeler

University of California, San Diego

David Plouffe

Genomics Institute of the Novartis Research Foundation

Kelli Kuhen

California Institute for Biomedical Research

Richard Glynne

Genomics Institute of the Novartis Research Foundation

Thierry T. Diagana

Novartis (United States)

Cooperative Institutions

Genomics Institute of the Novartis Research Foundation

111

Novartis (Singapore)

Novartis (Switzerland)

Scripps Research Institute

University of Basel

Swiss Tropical and Public Health Institute

Novartis (United States)

Boston Biomedical Research Institute

University of South Florida

Novartis Institutes for BioMedical Research

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Metal Salts of Thiocarbonic Acid -Monoesters and -Monoesters

Four Carbon-Heteroatom Bonds (2005)

K. W. Jung A. S. Nagle

10.1055/sos-sd-018-00459

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Formal Aromatic C−H Insertion for Stereoselective Isoquinolinone Synthesis and Studies on Mechanistic Insights into the C−C Bond Formation

The Journal of Organic Chemistry (2009)

Chan Pil Park A. S. Nagle Cheol Hwan Yoon Chiliu Chen Kyung Woon Jung

Formal aromatic C-H insertion of rhodium(II) carbenoid was intensively investigated to develop a new methodology and probe its mechanism. Contrasting with the previously proposed direct C-H insertion, the mechanism was revealed to be electrophilic aromatic substitution, which was supported by substituent effects on the aromatic ring and a secondary deuterium kinetic isotope effect. Various isoquinolinones were synthesized intramolecularly via six-membered ring formation with high regio- and diastereoselectivity, while averting the common Buchner-type reaction. Intermolecularly, dirhodium catalyzed formal aromatic C-H insertion on electron-rich aromatics was also achieved.

Carbenoid

Electrophilic aromatic substitution

Insertion reaction

Electrophilic substitution

Electrophilic addition

Isoquinoline

10.1021/jo9011255

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Citations (64)

Acyclic Thiocarbonate ,-Diesters

Four Carbon-Heteroatom Bonds (2005)

K. W. Jung A. S. Nagle

10.1055/sos-sd-018-00463

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Hydrolysis of Ammonium Salts

Four Carbon-Heteroatom Bonds (2005)

K. W. Jung A. S. Nagle

10.1055/sos-sd-018-00473

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Synthesis of Product Subclass 20

Four Carbon-Heteroatom Bonds (2005)

K. W. Jung A. S. Nagle

Subclass

10.1055/sos-sd-018-00480

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Acyclic Carbonate Diesters

Four Carbon-Heteroatom Bonds (2005)

K. W. Jung A. S. Nagle

10.1055/sos-sd-018-00404

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Disease Transmission Prophylaxis, Treatment, and Prevention of Candidate with Potential for Use in KAF156 Is an Antimalarial Clinical

Thierry T. Diagana Elizabeth A. Winzeler Richard Glynne Joseph M. Vinetz Laurent Rénia

Antimicrob. Agents Chemother.€2014, 58(9):5060. DOI:Thierry T. DiaganaSauerwein, Elizabeth A. Winzeler, Richard J. Glynne and Flannery, Joseph M. Vinetz, Laurent Renia, Robert W.John R. Walker, David Tully, Kailash P. Patra, Erika L. Gettayacamin, Jetsumon Sattabongkot, Jennifer Taylor,Price, Francois Nosten, Anchalee Tungtaeng, Montip Jutta Marfurt, Bruce Russell, Rossarin Suwanarusk, Ric N.Geert J. van Gemert, Grennady Wirjanata, Boni Sebayang, Fidock, Wouter Graumans, Marga van de Vegte-Bolmer,Whitney Barnes, David Plouffe, Marcus C. S. Lee, David A. Zhong Chen, Carolyn Francek, Tao Wu, Advait Nagle, S.Kerstin Gagaring, Rachel Borboa, Jennifer Buenviaje, Kelli L. Kuhen, Arnab K. Chatterjee, Matthias Rottmann,€

Flannery

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Isomerization of Dithiocarbonate ,-Diesters

Four Carbon-Heteroatom Bonds (2005)

K. W. Jung A. S. Nagle

10.1055/sos-sd-018-00527

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Lead Optimization of Imidazopyrazines: A New Class of Antimalarial with Activity on Plasmodium Liver Stages

ACS Medicinal Chemistry Letters (2014)

Bin Zou A. S. Nagle Arnab K. Chatterjee Seh Yong Leong Liying Jocelyn Tan

Imidazopyridine 1 was identified from a phenotypic screen against P. falciparum (Pf) blood stages and subsequently optimized for activity on liver-stage schizonts of the rodent parasite P. yoelii (Py) as well as hypnozoites of the simian parasite P. cynomolgi (Pc). We applied these various assays to the cell-based lead optimization of the imidazopyrazines, exemplified by 3 (KAI407), and show that optimized compounds within the series with improved pharmacokinetic properties achieve causal prophylactic activity in vivo and may have the potential to target the dormant stages of P. vivax malaria.

Plasmodium (life cycle)

10.1021/ml500244m

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Citations (31)

Synthesis of Product Subclass 30

Four Carbon-Heteroatom Bonds (2005)

K. W. Jung A. S. Nagle

Subclass

10.1055/sos-sd-018-00512

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