Search Results - "STREET, LESLIE J" :: K.UTB vyhledávací portál | TBU Library Retrieval Portal

Medicinal Chemistry Optimization of Antiplasmodial Imidazopyridazine Hits from High Throughput Screening of a SoftFocus Kinase Library: Part 1

Medicinal Chemistry Optimization of Antiplasmodial Imidazopyridazine Hits from High Throughput Screening of a SoftFocus Kinase Library: Part 1

by Le Manach, Claire, Gonzàlez Cabrera, Diego, Douelle, Frederic, Nchinda, Aloysius T, Younis, Yassir, Taylor, Dale, Wiesner, Lubbe, White, Karen L, Ryan, Eileen, March, Corinne, Duffy, Sandra, Avery, Vicky M, Waterson, David, Witty, Michael J, Wittlin, Sergio, Charman, Susan A, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (27.03.2014)

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Imidazo[1,2-a]pyrimidines as Functionally Selective and Orally Bioavailable GABAAα2/α3 Binding Site Agonists for the Treatment of Anxiety Disorders

Imidazo[1,2-a]pyrimidines as Functionally Selective and Orally Bioavailable GABAAα2/α3 Binding Site Agonists for the Treatment of Anxiety Disorders

by Goodacre, Simon C, Street, Leslie J, Hallett, David J, Crawforth, James M, Kelly, Sarah, Owens, Andrew P, Blackaby, Wesley P, Lewis, Richard T, Stanley, Joanna, Smith, Alison J, Ferris, Pushpinder, Sohal, Bindi, Cook, Susan M, Pike, Andrew, Brown, Nicola, Wafford, Keith A, Marshall, George, Castro, José L, Atack, John R
Published in Journal of medicinal chemistry (12.01.2006)

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Lerisetron Analogues with Antimalarial Properties: Synthesis, Structure–Activity Relationship Studies, and Biological Assessment

Lerisetron Analogues with Antimalarial Properties: Synthesis, Structure–Activity Relationship Studies, and Biological Assessment

by Mueller, Rudolf, Reddy, Virsinha, Nchinda, Aloysius T, Mebrahtu, Fanuel, Taylor, Dale, Lawrence, Nina, Tanner, Lloyd, Barnabe, Marine, Eyermann, Charles J, Zou, Bin, Kondreddi, Ravinder R, Lakshminarayana, Suresh B, Rottmann, Matthias, Street, Leslie J, Chibale, Kelly
Published in ACS omega (31.03.2020)

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$Dose-fractionation studies of a Plasmodium phosphatidylinositol 4-kinase inhibitor in a humanized mouse model of malaria$

Dose-fractionation studies of a Plasmodium phosphatidylinositol 4-kinase inhibitor in a humanized mouse model of malaria

by Gibhard, Liezl, Njoroge, Mathew, Mulubwa, Mwila, Lawrence, Nina, Smith, Dennis, Duffy, James, Le Manach, Claire, Brunschwig, Christel, Taylor, Dale, van der Westhuyzen, Renier, Street, Leslie J, Basarab, Gregory S, Chibale, Kelly
Published in Antimicrobial agents and chemotherapy (08.10.2024)

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Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria

Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria

by Kandepedu, Nishanth, Gonzàlez Cabrera, Diego, Eedubilli, Srinivas, Taylor, Dale, Brunschwig, Christel, Gibhard, Liezl, Njoroge, Mathew, Lawrence, Nina, Paquet, Tanya, Eyermann, Charles J, Spangenberg, Thomas, Basarab, Gregory S, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (12.07.2018)

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Pyrrolo[3,4‑c]pyridine-1,3(2H)‑diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration

Pyrrolo[3,4‑c]pyridine-1,3(2H)‑diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration

by van der Westhuyzen, Renier, Winks, Susan, Wilson, Colin R, Boyle, Grant A, Gessner, Richard K, Soares de Melo, Candice, Taylor, Dale, de Kock, Carmen, Njoroge, Mathew, Brunschwig, Christel, Lawrence, Nina, Rao, Srinivasa P.S, Sirgel, Frederick, van Helden, Paul, Seldon, Ronnett, Moosa, Atica, Warner, Digby F, Arista, Luca, Manjunatha, Ujjini H, Smith, Paul W, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (10.12.2015)

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Benzoheterocyclic Oxime Carbamates Active against Mycobacterium tuberculosis: Synthesis, Structure–Activity Relationship, Metabolism, and Biology Triaging

Benzoheterocyclic Oxime Carbamates Active against Mycobacterium tuberculosis: Synthesis, Structure–Activity Relationship, Metabolism, and Biology Triaging

by van der Westhuyzen, Renier, Mabhula, Amanda, Njaria, Paul M, Müller, Rudolf, Ngumbu Muhunga, Denis, Taylor, Dale, Lawrence, Nina, Njoroge, Mathew, Brunschwig, Christel, Moosa, Atica, Singh, Vinayak, Rao, Srinivasa P.S, Manjunatha, Ujjini H, Smith, Paul W, Warner, Digby F, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (08.07.2021)

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Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model

Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model

by Horatscheck, André, Andrijevic, Ana, Nchinda, Aloysius T, Le Manach, Claire, Paquet, Tanya, Khonde, Lutete Peguy, Dam, Jean, Pawar, Kailash, Taylor, Dale, Lawrence, Nina, Brunschwig, Christel, Gibhard, Liezl, Njoroge, Mathew, Reader, Janette, van der Watt, Mariëtte, Wicht, Kathryn, de Sousa, Ana Carolina C, Okombo, John, Maepa, Keletso, Egan, Timothy J, Birkholtz, Lyn-Marie, Basarab, Gregory S, Wittlin, Sergio, Fish, Paul V, Street, Leslie J, Duffy, James, Chibale, Kelly
Published in Journal of medicinal chemistry (12.11.2020)

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Investigating Sulfoxide-to-Sulfone Conversion as a Prodrug Strategy for a Phosphatidylinositol 4-Kinase Inhibitor in a Humanized Mouse Model of Malaria

Investigating Sulfoxide-to-Sulfone Conversion as a Prodrug Strategy for a Phosphatidylinositol 4-Kinase Inhibitor in a Humanized Mouse Model of Malaria

by Gibhard, Liezl, Njoroge, Mathew, Paquet, Tanya, Brunschwig, Christel, Taylor, Dale, Lawrence, Nina, Abay, Efrem, Wittlin, Sergio, Wiesner, Lubbe, Street, Leslie J, Chibale, Kelly, Basarab, Gregory S
Published in Antimicrobial agents and chemotherapy (01.12.2018)

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Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of GlyT1

Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of GlyT1

by Blackaby, Wesley P, Lewis, Richard T, Thomson, Joanne L, Jennings, Andrew S. R, Goodacre, Simon C, Street, Leslie J, MacLeod, Angus M, Pike, Andrew, Wood, Suzanne, Thomas, Steve, Brown, Terry A, Smith, Alison, Pillai, Gopalan, Almond, Sarah, Guscott, Martin R, Burns, H. Donald, Eng, Waisi, Ryan, Christine, Cook, Jacquelynn, Hamill, Terence G
Published in ACS medicinal chemistry letters (14.10.2010)

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Aminopyrazolo[1,5-a]pyrimidines as potential inhibitors of Mycobacterium tuberculosis: Structure activity relationships and ADME characterization

Aminopyrazolo[1,5-a]pyrimidines as potential inhibitors of Mycobacterium tuberculosis: Structure activity relationships and ADME characterization

by Soares de Melo, Candice, Feng, Tzu-Shean, van der Westhuyzen, Renier, Gessner, Richard K., Street, Leslie J., Morgans, Garreth L., Warner, Digby F., Moosa, Atica, Naran, Krupa, Lawrence, Nina, Boshoff, Helena I.M., Barry, Clifton E., Harris, C. John, Gordon, Richard, Chibale, Kelly
Published in Bioorganic & medicinal chemistry (15.11.2015)

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Identification of a Potential Antimalarial Drug Candidate from a Series of 2‑Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle

Identification of a Potential Antimalarial Drug Candidate from a Series of 2‑Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle

by Le Manach, Claire, Nchinda, Aloysius T, Paquet, Tanya, Gonzàlez Cabrera, Diego, Younis, Yassir, Han, Ze, Bashyam, Sridevi, Zabiulla, Mohammed, Taylor, Dale, Lawrence, Nina, White, Karen L, Charman, Susan A, Waterson, David, Witty, Michael J, Wittlin, Sergio, Botha, Mariëtte E, Nondaba, Sindisiswe H, Reader, Janette, Birkholtz, Lyn-Marie, Jiménez-Díaz, María Belén, Martínez, María Santos, Ferrer, Santiago, Angulo-Barturen, Iñigo, Meister, Stephan, Antonova-Koch, Yevgeniya, Winzeler, Elizabeth A, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (10.11.2016)

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Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose–Response Curves against Multidrug Resistant Parasite Strains

Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose–Response Curves against Multidrug Resistant Parasite Strains

by Le Manach, Claire, Paquet, Tanya, Wicht, Kathryn, Nchinda, Aloysius T, Brunschwig, Christel, Njoroge, Mathew, Gibhard, Liezl, Taylor, Dale, Lawrence, Nina, Wittlin, Sergio, Eyermann, Charles J, Basarab, Gregory S, Duffy, James, Fish, Paul V, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (25.10.2018)

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Medicinal Chemistry Optimization of Antiplasmodial Imidazopyridazine Hits from High Throughput Screening of a SoftFocus Kinase Library: Part 2

Medicinal Chemistry Optimization of Antiplasmodial Imidazopyridazine Hits from High Throughput Screening of a SoftFocus Kinase Library: Part 2

by Le Manach, Claire, Paquet, Tanya, Gonzàlez Cabrera, Diego, Younis, Yassir, Taylor, Dale, Wiesner, Lubbe, Lawrence, Nina, Schwager, Sylva, Waterson, David, Witty, Michael J, Wittlin, Sergio, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (13.11.2014)

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Cell-based medicinal chemistry optimization of high throughput screening hits for orally active antimalarials. Part 2: hits from SoftFocus kinase and other libraries

Cell-based medicinal chemistry optimization of high throughput screening hits for orally active antimalarials. Part 2: hits from SoftFocus kinase and other libraries

by Younis, Yassir, Street, Leslie J, Waterson, David, Witty, Michael J, Chibale, Kelly
Published in Journal of medicinal chemistry (24.10.2013)

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Novel Antitubercular 6‑Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure–Activity Relationship and Target Identification Studies

Novel Antitubercular 6‑Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure–Activity Relationship and Target Identification Studies

by Wilson, Colin R, Gessner, Richard K, Moosa, Atica, Seldon, Ronnett, Warner, Digby F, Mizrahi, Valerie, Soares de Melo, Candice, Simelane, Sandile B, Nchinda, Aloysius, Abay, Efrem, Taylor, Dale, Njoroge, Mathew, Brunschwig, Christel, Lawrence, Nina, Boshoff, Helena I. M, Barry, Clifton E, Sirgel, Frederick A, van Helden, Paul, Harris, C. John, Gordon, Richard, Ghidelli-Disse, Sonja, Pflaumer, Hannah, Boesche, Markus, Drewes, Gerard, Sanz, Olalla, Santos, Gracia, Rebollo-Lopez, Maria José, Urones, Beatriz, Selenski, Carolyn, Lafuente-Monasterio, Maria Jose, Axtman, Matthew, Lelièvre, Joël, Ballell, Lluis, Mueller, Rudolf, Street, Leslie J, Ghorpade, Sandeep R, Chibale, Kelly
Published in Journal of medicinal chemistry (28.12.2017)

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Correction to “Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model”

Correction to “Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model”

by Horatscheck, André, Andrijevic, Ana, Nchinda, Aloysius T, Le Manach, Claire, Paquet, Tanya, Khonde, Lutete Peguy, Dam, Jean, Pawar, Kailash, Taylor, Dale, Lawrence, Nina, Brunschwig, Christel, Gibhard, Liezl, Njoroge, Mathew, Reader, Janette, van der Watt, Mariëtte, Wicht, Kathryn, de Sousa, Ana Carolina C, Okombo, John, Maepa, Keletso, Egan, Timothy J, Birkholtz, Lyn-Marie, Basarab, Gregory S, Wittlin, Sergio, Fish, Paul V, Street, Leslie J, Duffy, James, Chibale, Kelly
Published in Journal of medicinal chemistry (11.02.2021)

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A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum -Infected Mouse Models from Structure–Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines

A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum -Infected Mouse Models from Structure–Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines

by Le Manach, Claire, Paquet, Tanya, Brunschwig, Christel, Njoroge, Mathew, Han, Ze, Gonzàlez Cabrera, Diego, Bashyam, Sridevi, Dhinakaran, Rajkumar, Taylor, Dale, Reader, Janette, Botha, Mariette, Churchyard, Alisje, Lauterbach, Sonja, Coetzer, Theresa L, Birkholtz, Lyn-Marie, Meister, Stephan, Winzeler, Elizabeth A, Waterson, David, Witty, Michael J, Wittlin, Sergio, Jiménez-Díaz, María-Belén, Santos Martínez, María, Ferrer, Santiago, Angulo-Barturen, Iñigo, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (12.11.2015)

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Synthesis and biological evaluation of aryl-oxadiazoles as inhibitors of Mycobacterium tuberculosis

Synthesis and biological evaluation of aryl-oxadiazoles as inhibitors of Mycobacterium tuberculosis

by Martinez-Grau, Maria Angeles, Valcarcel, Isabel C. Gonzalez, Early, Julie V., Gessner, Richard Klaus, de Melo, Candice Soares, de la Nava, Eva Maria Martin, Korkegian, Aaron, Ovechkina, Yulia, Flint, Lindsay, Gravelle, Anisa, Cramer, Jeff W., Desai, Prashant V., Street, Leslie J., Odingo, Joshua, Masquelin, Thierry, Chibale, Kelly, Parish, Tanya
Published in Bioorganic & medicinal chemistry letters (01.06.2018)

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Potent Plasmodium falciparum gametocytocidal compounds identified by exploring the kinase inhibitor chemical space for dual active antimalarials

Potent Plasmodium falciparum gametocytocidal compounds identified by exploring the kinase inhibitor chemical space for dual active antimalarials

by van der Watt, Mariëtte E, Reader, Janette, Churchyard, Alisje, Nondaba, Sindisiwe H, Lauterbach, Sonja B, Niemand, Jandeli, Abayomi, Sijuade, van Biljon, Riëtte A, Connacher, Jessica I, van Wyk, Roelof D J, Le Manach, Claire, Paquet, Tanya, González Cabrera, Diego, Brunschwig, Christel, Theron, Anjo, Lozano-Arias, Sonia, Rodrigues, Janneth F I, Herreros, Esperanza, Leroy, Didier, Duffy, James, Street, Leslie J, Chibale, Kelly, Mancama, Dalu, Coetzer, Theresa L, Birkholtz, Lyn-Marie
Published in Journal of antimicrobial chemotherapy (01.05.2018)

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