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134 results on '"Nchinda, Aloysius"'

1. 1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in Mycobacterium tuberculosis

Author

Khonde, Lutete Peguy, Müller, Rudolf, Boyle, Grant A., Reddy, Virsinha, Nchinda, Aloysius T., Eyermann, Charles J., Fienberg, Stephen, Singh, Vinayak, Myrick, Alissa, Abay, Efrem, Njoroge, Mathew, Lawrence, Nina, Su, Qin, Myers, Timothy G., Boshoff, Helena I. M., Barry, Clifton E., Sirgel, Frederick A., van Helden, Paul D., Massoudi, Lisa M., Robertson, Gregory T., Lenaerts, Anne J., Basarab, Gregory S., Ghorpade, Sandeep R., and Chibale, Kelly

Abstract

This is the accepted manuscript version of the work published in its final form as Khonde, Lutete Peguy;Müller, Rudolf;Boyle, Grant A.;Reddy, Virsinha;Nchinda, Aloysius T.;Eyermann, Charles J.;Fienberg, Stephen;Singh, Vinayak;Myrick, Alissa;Abay, Efrem;Njoroge, Mathew;Lawrence, Nina;Su, Qin;Myers, Timothy G.;Boshoff, Helena I. M.;Barry, Clifton E.;Sirgel, Frederick A.;van Helden, Paul D.;Massoudi, Lisa M.;Robertson, Gregory T.;Lenaerts, Anne J.;Basarab, Gregory S.;Ghorpade, Sandeep R.;Chibale, Kelly. Journal of Medicinal Chemistry Volume: 64 issue: 17, page(s): 12790–12807.https://doi.org/10.1021/acs.jmedchem.1c00837 Deposited byshareyourpaper.organdopenaccessbutton.org. We've taken reasonable steps to ensure this content doesn't violate copyright. However, if you think it does you can request a takedown by emailinghelp@openaccessbutton.org.

Published
2021
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2. 1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in Mycobacterium tuberculosis

Author

Khonde, Lutete Peguy, primary, Müller, Rudolf, additional, Boyle, Grant A., additional, Reddy, Virsinha, additional, Nchinda, Aloysius T., additional, Eyermann, Charles J., additional, Fienberg, Stephen, additional, Singh, Vinayak, additional, Myrick, Alissa, additional, Abay, Efrem, additional, Njoroge, Mathew, additional, Lawrence, Nina, additional, Su, Qin, additional, Myers, Timothy G., additional, Boshoff, Helena I. M., additional, Barry, Clifton E., additional, Sirgel, Frederick A., additional, van Helden, Paul D., additional, Massoudi, Lisa M., additional, Robertson, Gregory T., additional, Lenaerts, Anne J., additional, Basarab, Gregory S., additional, Ghorpade, Sandeep R., additional, and Chibale, Kelly, additional

Published
2021
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3. Positional-scanning combinatorial libraries of fluorescence resonance energy transfer peptides for defining substrate specificity of the angiotensin I-converting enzyme and development of selective C-domain substrates

Author

Bersanetti, Patricia A., Andrade, Maria Claudina C., Casarini, Dulce E., Carmona, Adriana K., Juliano, Maria A., Juliano, Luiz, Nchinda, Aloysius T., and Sturrock, Edward D.

Subjects
Enzymes -- Chemical properties, Peptides -- Chemical properties, Energy transfer -- Research, Biological sciences, Chemistry
Abstract

The development of selective substrates for the C-domain of angiotensin 1-converting enzyme (ACE) using positional-scanning synthetic combinational (PS-SC) libraries of fluorescence resonance energy transfer peptides is described. It is concluded that the physiological functions of ACE are not limited to the cardiovascular system, and this has awakened an interest in defining the role of the enzyme and, more specifically, its N- and C-domain active sites in different biological processes.

Published
2004

6. 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”

Author

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

Published
2021
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7. 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

Author

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

Published
2020
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8. Synthesis, Structure–Activity Relationship, and Mechanistic Studies of Aminoquinazolinones Displaying Antimycobacterial Activity

Author

Akester, Jessica N., primary, Njaria, Paul, additional, Nchinda, Aloysius, additional, Le Manach, Claire, additional, Myrick, Alissa, additional, Singh, Vinayak, additional, Lawrence, Nina, additional, Njoroge, Mathew, additional, Taylor, Dale, additional, Moosa, Atica, additional, Smith, Anthony J., additional, Brooks, Elizabeth J., additional, Lenaerts, Anne J., additional, Robertson, Gregory T., additional, Ioerger, Thomas R., additional, Mueller, Rudolf, additional, and Chibale, Kelly, additional

Published
2020
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9. Lerisetron Analogues with Antimalarial Properties: Synthesis, Structure–Activity Relationship Studies, and Biological Assessment

Author

Mueller, Rudolf, primary, Reddy, Virsinha, additional, Nchinda, Aloysius T., additional, Mebrahtu, Fanuel, additional, Taylor, Dale, additional, Lawrence, Nina, additional, Tanner, Lloyd, additional, Barnabe, Marine, additional, Eyermann, Charles J., additional, Zou, Bin, additional, Kondreddi, Ravinder R., additional, Lakshminarayana, Suresh B., additional, Rottmann, Matthias, additional, Street, Leslie J., additional, and Chibale, Kelly, additional

Published
2020
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10. Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure–Activity Relationship and Target Identification Studies

Author

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, and Chibale, Kelly

Subjects
Male, Proteomics, Antitubercular Agents, Administration, Oral, Blood Proteins, Mycobacterium tuberculosis, Article, High-Throughput Screening Assays, Mice, Inbred C57BL, Small Molecule Libraries, Structure-Activity Relationship, Pyrimidines, Drug Stability, Microsomes, Liver, Animals, Humans
Abstract

A BioFocus DPI SoftFocus library of ∼35 000 compounds was screened against Mycobacterium tuberculosis (Mtb) in order to identify novel hits with antitubercular activity. The hits were evaluated in biology triage assays to exclude compounds suggested to function via frequently encountered promiscuous mechanisms of action including inhibition of the QcrB subunit of the cytochrome bc1 complex, disruption of cell-wall homeostasis, and DNA damage. Among the hits that passed this screening cascade, a 6-dialkylaminopyrimidine carboxamide series was prioritized for hit to lead optimization. Compounds from this series were active against clinical Mtb strains, while no cross-resistance to conventional antituberculosis drugs was observed. This suggested a novel mechanism of action, which was confirmed by chemoproteomic analysis leading to the identification of BCG_3193 and BCG_3827 as putative targets of the series with unknown function. Initial structure-activity relationship studies have resulted in compounds with moderate to potent antitubercular activity and improved physicochemical properties.

Published
2017

14. Erratum for Brunschwig et al., “UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria”

Author

Brunschwig, Christel, primary, Lawrence, Nina, additional, Taylor, Dale, additional, Abay, Efrem, additional, Njoroge, Mathew, additional, Basarab, Gregory S., additional, Le Manach, Claire, additional, Paquet, Tanya, additional, Gonzàlez Cabrera, Diego, additional, Nchinda, Aloysius T., additional, de Kock, Carmen, additional, Wiesner, Lubbe, additional, Denti, Paolo, additional, Waterson, David, additional, Blasco, Benjamin, additional, Leroy, Didier, additional, Witty, Michael J., additional, Donini, Cristina, additional, Duffy, James, additional, Wittlin, Sergio, additional, White, Karen L., additional, Charman, Susan A., additional, Jiménez-Díaz, Maria Belén, additional, Angulo-Barturen, Iñigo, additional, Herreros, Esperanza, additional, Gamo, Francisco Javier, additional, Rochford, Rosemary, additional, Mancama, Dalu, additional, Coetzer, Theresa L., additional, van der Watt, Mariëtte E., additional, Reader, Janette, additional, Birkholtz, Lyn-Marie, additional, Marsh, Kennan C., additional, Solapure, Suresh M., additional, Burke, John E., additional, McPhail, Jacob A., additional, Vanaerschot, Manu, additional, Fidock, David A., additional, Fish, Paul V., additional, Siegl, Peter, additional, Smith, Dennis A., additional, Wirjanata, Grennady, additional, Noviyanti, Rintis, additional, Price, Ric N., additional, Marfurt, Jutta, additional, Silue, Kigbafori D., additional, Street, Leslie J., additional, and Chibale, Kelly, additional

Published
2018
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15. 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

Author

Le Manach, Claire, primary, Paquet, Tanya, additional, Wicht, Kathryn, additional, Nchinda, Aloysius T., additional, Brunschwig, Christel, additional, Njoroge, Mathew, additional, Gibhard, Liezl, additional, Taylor, Dale, additional, Lawrence, Nina, additional, Wittlin, Sergio, additional, Eyermann, Charles J., additional, Basarab, Gregory S., additional, Duffy, James, additional, Fish, Paul V., additional, Street, Leslie J., additional, and Chibale, Kelly, additional

Published
2018
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16. UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria

Author

Brunschwig, Christel, primary, Lawrence, Nina, additional, Taylor, Dale, additional, Abay, Efrem, additional, Njoroge, Mathew, additional, Basarab, Gregory S., additional, Le Manach, Claire, additional, Paquet, Tanya, additional, Cabrera, Diego Gonzàlez, additional, Nchinda, Aloysius T., additional, de Kock, Carmen, additional, Wiesner, Lubbe, additional, Denti, Paolo, additional, Waterson, David, additional, Blasco, Benjamin, additional, Leroy, Didier, additional, Witty, Michael J., additional, Donini, Cristina, additional, Duffy, James, additional, Wittlin, Sergio, additional, White, Karen L., additional, Charman, Susan A., additional, Jiménez-Díaz, Maria Belén, additional, Angulo-Barturen, Iñigo, additional, Herreros, Esperanza, additional, Gamo, Francisco Javier, additional, Rochford, Rosemary, additional, Mancama, Dalu, additional, Coetzer, Theresa L., additional, van der Watt, Mariëtte E., additional, Reader, Janette, additional, Birkholtz, Lyn-Marie, additional, Marsh, Kennan C., additional, Solapure, Suresh M., additional, Burke, John E., additional, McPhail, Jacob A., additional, Vanaerschot, Manu, additional, Fidock, David A., additional, Fish, Paul V., additional, Siegl, Peter, additional, Smith, Dennis A., additional, Wirjanata, Grennady, additional, Noviyanti, Rintis, additional, Price, Ric N., additional, Marfurt, Jutta, additional, Silue, Kigbafori D., additional, Street, Leslie J., additional, and Chibale, Kelly, additional

Published
2018
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17. Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγnull Mouse Model of Malaria

Author

Nchinda, Aloysius T., primary, Le Manach, Claire, additional, Paquet, Tanya, additional, Gonzàlez Cabrera, Diego, additional, Wicht, Kathryn J., additional, Brunschwig, Christel, additional, Njoroge, Mathew, additional, Abay, Efrem, additional, Taylor, Dale, additional, Lawrence, Nina, additional, Wittlin, Sergio, additional, Jiménez-Díaz, María-Belén, additional, Santos Martínez, María, additional, Ferrer, Santiago, additional, Angulo-Barturen, Iñigo, additional, Lafuente-Monasterio, Maria Jose, additional, Duffy, James, additional, Burrows, Jeremy, additional, Street, Leslie J., additional, and Chibale, Kelly, additional

Published
2018
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18. Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In VivoEfficacy in the Plasmodium falciparumNSG Mouse Model

Author

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, and Chibale, Kelly

Abstract

A series of 2,4-disubstituted imidazopyridines, originating from a SoftFocus Kinase library, was identified from a high throughput phenotypic screen against the human malaria parasite Plasmodium falciparum. Hit compounds showed moderate asexual blood stage activity. During lead optimization, several issues were flagged such as cross-resistance against the multidrug-resistant K1 strain, in vitrocytotoxicity, and cardiotoxicity and were addressed through structure–activity and structure–property relationship studies. Pharmacokinetic properties were assessed in mice for compounds showing desirable in vitroactivity, a selectivity window over cytotoxicity, and microsomal metabolic stability. Frontrunner compound 37showed good exposure in mice combined with good in vitroactivity against the malaria parasite, which translated into in vivoefficacy in the P. falciparumNOD-scid IL-2Rγnull(NSG) mouse model. Preliminary mechanistic studies suggest inhibition of hemozoin formation as a contributing mode of action.

Published
2020
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19. 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

Author

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

Published
2016
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20. Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγnull Mouse Model of Malaria.

Author

Nchinda, Aloysius T., Le Manach, Claire, Paquet, Tanya, Cabrera, Diego Gonzàlez, Wicht, Kathryn J., Brunschwig, Christel, Njoroge, Mathew, Abay, Efrem, Taylor, Dale, Lawrence, Nina, Wittlin, Sergio, Jiménez-Díaz, María-Belén, Martínez, María Santos, Ferrer, Santiago, Angulo-Barturen, Iñigo, Lafuente-Monasterio, Maria Jose, Duffy, James, Burrows, Jeremy, Street, Leslie J., and Chibale, Kelly

Subjects
*IMIDAZOPYRIDINES, *PLASMODIUM falciparum, *MALARIA, *METABOLISM, *PHENOTYPES
Abstract

Optimization of a chemical series originating from whole-cell phenotypic screening against the human malaria parasite, Plasmodium falciparum, led to the identification of two promising 2,6-disubstituted imidazopyridine compounds, 43 and 74. These compounds exhibited potent activity against asexual blood stage parasites that, together with their in vitro absorption, distribution, metabolism, and excretion (ADME) properties, translated to in vivo efficacy with clearance of parasites in the PfSCID mouse model for malaria within 48 h of treatment. [ABSTRACT FROM AUTHOR]

Published
2018
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21. Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure–Activity Relationship and Target Identification Studies

Author

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., and Chibale, Kelly

Abstract

A BioFocus DPI SoftFocus library of ∼35 000 compounds was screened against Mycobacterium tuberculosis(Mtb) in order to identify novel hits with antitubercular activity. The hits were evaluated in biology triage assays to exclude compounds suggested to function via frequently encountered promiscuous mechanisms of action including inhibition of the QcrB subunit of the cytochrome bc1complex, disruption of cell–wall homeostasis, and DNA damage. Among the hits that passed this screening cascade, a 6-dialkylaminopyrimidine carboxamide series was prioritized for hit to lead optimization. Compounds from this series were active against clinical Mtb strains, while no cross-resistance to conventional antituberculosis drugs was observed. This suggested a novel mechanism of action, which was confirmed by chemoproteomic analysis leading to the identification of BCG_3193 and BCG_3827 as putative targets of the series with unknown function. Initial structure–activity relationship studies have resulted in compounds with moderate to potent antitubercular activity and improved physicochemical properties.

Published
2024
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22. Medicinal Chemistry Optimization of Antiplasmodial Imidazopyridazine Hits from High Throughput Screening of a SoftFocus Kinase Library: Part 1

Author

Le Manach, Claire, primary, Gonzàlez Cabrera, Diego, additional, Douelle, Frederic, additional, Nchinda, Aloysius T., additional, Younis, Yassir, additional, Taylor, Dale, additional, Wiesner, Lubbe, additional, White, Karen L., additional, Ryan, Eileen, additional, March, Corinne, additional, Duffy, Sandra, additional, Avery, Vicky M., additional, Waterson, David, additional, Witty, Michael J., additional, Wittlin, Sergio, additional, Charman, Susan A., additional, Street, Leslie J., additional, and Chibale, Kelly, additional

Published
2014
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23. 2,4-Diaminothienopyrimidines as Orally Active Antimalarial Agents

Author

González Cabrera, Diego, primary, Le Manach, Claire, additional, Douelle, Frederic, additional, Younis, Yassir, additional, Feng, Tzu-Shean, additional, Paquet, Tanya, additional, Nchinda, Aloysius T., additional, Street, Leslie J., additional, Taylor, Dale, additional, de Kock, Carmen, additional, Wiesner, Lubbe, additional, Duffy, Sandra, additional, White, Karen L., additional, Zabiulla, K. Mohammed, additional, Sambandan, Yuvaraj, additional, Bashyam, Sridevi, additional, Waterson, David, additional, Witty, Michael J., additional, Charman, Susan A., additional, Avery, Vicky M., additional, Wittlin, Sergio, additional, and Chibale, Kelly, additional

Published
2014
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24. Structure–Activity-Relationship Studies around the 2-Amino Group and Pyridine Core of Antimalarial 3,5-Diarylaminopyridines Lead to a Novel Series of Pyrazine Analogues with Oral in Vivo Activity

Author

Younis, Yassir, primary, Douelle, Frederic, additional, González Cabrera, Diego, additional, Le Manach, Claire, additional, Nchinda, Aloysius T., additional, Paquet, Tanya, additional, Street, Leslie J., additional, White, Karen L., additional, Zabiulla, K. Mohammed, additional, Joseph, Jayan T., additional, Bashyam, Sridevi, additional, Waterson, David, additional, Witty, Michael J., additional, Wittlin, Sergio, additional, Charman, Susan A., additional, and Chibale, Kelly, additional

Published
2013
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25. Structure–Activity Relationship Studies of Orally Active Antimalarial 3,5-Substituted 2-Aminopyridines

Author

González Cabrera, Diego, primary, Douelle, Frederic, additional, Younis, Yassir, additional, Feng, Tzu-Shean, additional, Le Manach, Claire, additional, Nchinda, Aloysius T., additional, Street, Leslie J., additional, Scheurer, Christian, additional, Kamber, Jolanda, additional, White, Karen L., additional, Montagnat, Oliver D., additional, Ryan, Eileen, additional, Katneni, Kasiram, additional, Zabiulla, K. Mohammed, additional, Joseph, Jayan T., additional, Bashyam, Sridevi, additional, Waterson, David, additional, Witty, Michael J., additional, Charman, Susan A., additional, Wittlin, Sergio, additional, and Chibale, Kelly, additional

Published
2012
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26. 3,5-Diaryl-2-aminopyridines as a Novel Class of Orally Active Antimalarials Demonstrating Single Dose Cure in Mice and Clinical Candidate Potential

Author

Younis, Yassir, primary, Douelle, Frederic, additional, Feng, Tzu-Shean, additional, Cabrera, Diego González, additional, Manach, Claire Le, additional, Nchinda, Aloysius T., additional, Duffy, Sandra, additional, White, Karen L., additional, Shackleford, David M., additional, Morizzi, Julia, additional, Mannila, Janne, additional, Katneni, Kasiram, additional, Bhamidipati, Ravi, additional, Zabiulla, K. Mohammed, additional, Joseph, Jayan T., additional, Bashyam, Sridevi, additional, Waterson, David, additional, Witty, Michael J., additional, Hardick, David, additional, Wittlin, Sergio, additional, Avery, Vicky, additional, Charman, Susan A., additional, and Chibale, Kelly, additional

Published
2012
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27. Novel Orally Active Antimalarial Thiazoles

Author

González Cabrera, Diego, primary, Douelle, Frederic, additional, Feng, Tzu-Shean, additional, Nchinda, Aloysius T., additional, Younis, Yassir, additional, White, Karen L., additional, Wu, Quoc, additional, Ryan, Eileen, additional, Burrows, Jeremy N., additional, Waterson, David, additional, Witty, Michael J., additional, Wittlin, Sergio, additional, Charman, Susan A., additional, and Chibale, Kelly, additional

Published
2011
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40. Medicinal Chemistry Optimizationof AntiplasmodialImidazopyridazine Hits from High Throughput Screening of a SoftFocusKinase Library: Part 1.

Author

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., and Chibale, Kelly

Published
2014
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41. 2,4-Diaminothienopyrimidinesas Orally Active AntimalarialAgents.

Author

González Cabrera, Diego, Le Manach, Claire, Douelle, Frederic, Younis, Yassir, Feng, Tzu-Shean, Paquet, Tanya, Nchinda, Aloysius T., Street, Leslie J., Taylor, Dale, de Kock, Carmen, Wiesner, Lubbe, Duffy, Sandra, White, Karen L., Zabiulla, K. Mohammed, Sambandan, Yuvaraj, Bashyam, Sridevi, Waterson, David, Witty, Michael J., Charman, Susan A., and Avery, Vicky M.

Published
2014
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42. Structure–Activity-RelationshipStudies aroundthe 2-Amino Group and Pyridine Core of Antimalarial 3,5-DiarylaminopyridinesLead to a Novel Series of Pyrazine Analogues with Oral in Vivo Activity.

Author

Younis, Yassir, Douelle, Frederic, González Cabrera, Diego, Le Manach, Claire, Nchinda, Aloysius T., Paquet, Tanya, Street, Leslie J., White, Karen L., Zabiulla, K. Mohammed, Joseph, Jayan T., Bashyam, Sridevi, Waterson, David, Witty, Michael J., Wittlin, Sergio, Charman, Susan A., and Chibale, Kelly

Published
2013
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43. Structure–ActivityRelationship Studies ofOrally Active Antimalarial 3,5-Substituted 2-Aminopyridines.

Author

González Cabrera, Diego, Douelle, Frederic, Younis, Yassir, Feng, Tzu-Shean, Le Manach, Claire, Nchinda, Aloysius T., Street, Leslie J., Scheurer, Christian, Kamber, Jolanda, White, Karen L., Montagnat, Oliver D., Ryan, Eileen, Katneni, Kasiram, Zabiulla, K. Mohammed, Joseph, Jayan T., Bashyam, Sridevi, Waterson, David, Witty, Michael J., Charman, Susan A., and Wittlin, Sergio

Published
2012
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45. Chromone Studies. Part 11.1Synthesis and Electron-Impact Mass Spectrometric Study of Granulosin and Side-Chain Analogues†

Author

Kaye, Perry T., Nchinda, Aloysius T., and Gray, Christopher A.

Abstract

Granulosin, a chromone constituent of the bark of Galipea granulosa, and four analogues, all of which exhibit toxicity to the brine shrimp Artemia salina, have been prepared from 2′,3′,4′-trihydroxyacetophenone. High-resolution mass spectrometric analysis has permitted elucidation of the fragmentation patterns exhibited by these systems following electron-impact ionisation.

Published
2002
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47. Correction to “Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In VivoEfficacy in the Plasmodium falciparumNSG Mouse Model”

Author

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, and Chibale, Kelly

Published
2021
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48. Chromone Studies. Part 14.1Unprecedented Dimerisation of Chromone-3-Carbaldehyde-Derived Baylis–Hillman Adducts

Author

Kaye, Perry T., Nchinda, Aloysius T., Sabbagh, Liezel V., and Bacsa, John

Abstract

1,4-Diazabicyclo[2.2.2]octane (DABCO)-catalysed Baylis-Hillman reactions of selected chromone-3-carbaldehydes with methyl acrylate have been shown to afford mixtures of the expected Baylis-Hillman products and unprecedented dimeric derivatives. The Baylis–Hillman products, on heating at 80°C in the presence of DABCO, are converted to the corresponding dimers, the structures of which have been unambiguously established by NMR and X-ray crystallographic analysis. Electron-impact and electrospray MS data for the dimeric systems are discussed.

Published
2003
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49. Chromone studies. Part 10.1Substituent effects on the basicity of 2-(N,N-dimethylamino)chromones†

Author

Kaye, Perry T., Nchinda, Aloysius T., Sabbagh, Liezel V., and McCleland, Cedric W.

Abstract

The pKavalues for a series of 12, substituted 2-(N,N-dimethylamino)chromones have been determined by potentiometric titration and found to lie within a narrow range (1.92–2.52), protonation of the carbonyl oxygen being supported by 13C NMR data and semi-empirical and ab initio calculations.

Published
2000
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50. Erratum for Brunschwig et al., “UCT943, a Next-Generation Plasmodium falciparumPI4K Inhibitor Preclinical Candidate for the Treatment of Malaria”

Author

Brunschwig, Christel, Lawrence, Nina, Taylor, Dale, Abay, Efrem, Njoroge, Mathew, Basarab, Gregory S., Le Manach, Claire, Paquet, Tanya, Gonzàlez Cabrera, Diego, Nchinda, Aloysius T., de Kock, Carmen, Wiesner, Lubbe, Denti, Paolo, Waterson, David, Blasco, Benjamin, Leroy, Didier, Witty, Michael J., Donini, Cristina, Duffy, James, Wittlin, Sergio, White, Karen L., Charman, Susan A., Jiménez-Díaz, Maria Belén, Angulo-Barturen, Iñigo, Herreros, Esperanza, Gamo, Francisco Javier, Rochford, Rosemary, Mancama, Dalu, Coetzer, Theresa L., van der Watt, Mariëtte E., Reader, Janette, Birkholtz, Lyn-Marie, Marsh, Kennan C., Solapure, Suresh M., Burke, John E., McPhail, Jacob A., Vanaerschot, Manu, Fidock, David A., Fish, Paul V., Siegl, Peter, Smith, Dennis A., Wirjanata, Grennady, Noviyanti, Rintis, Price, Ric N., Marfurt, Jutta, Silue, Kigbafori D., Street, Leslie J., and Chibale, Kelly

Published
2018
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