Structure−activity relationship studies reveal new astemizole analogues active against Plasmodium falciparum in vitro

Structure-Activity Relationships of Antiplasmodial Pantothenamide Analogues Reveal a New Way by Which Triazoles Mimic Amide Bonds

Guan, Jinming
Tjhin, Erick
Howieson, Vanessa
Kittikool, Tanakorn
Spry, Christina
Saliba, Kevin
Auclair, Karine

March 2019

Pantothenamides are potent growth inhibitors of the malaria parasite Plasmodium falciparum. Their cl...

New active drugs against liver stages of Plasmodium predicted by molecular topology.

Mahmoudi, N.
Garcia-Domenech, R.
Galvez, J.
Farhati, K.
Franetich, J.F.
Sauerwein, R.W.
Hannoun, L.
Derouin, F.
Danis, M.
Mazier, D.

January 2008

Item does not contain fulltextWe conducted a quantitative structure-activity relationship (QSAR) stu...

Antimalarial agents against both sexual and asexual parasites stages: structure-activity relationships and biological studies of the Malaria Box compound 1-[5-(4-bromo-2-chlorophenyl)furan-2-yl]-N-[(piperidin-4-yl)methyl]methanamine (MMV019918) and analogues

A. Vallone
S. D&apos
S. Brogi
M. Brindisi
G. Chemi
G. Alfano
S. Lamponi
S.G. Lee
J.M. Jez
K.J.M. Koolen
K.J. Dechering
S. Saponara
F. Fusi
B. Gorelli
D. Taramelli
S. Parapini
R. Caldelari
G. Campiani
S. Gemma
S. Butini

March 2018

Therapies addressing multiple stages of Plasmodium falciparum life cycle are highly desirable for im...

Multistage antiplasmodium activity of astemizole analogues and inhibition of hemozoin formation as a contributor to their mode of action

Kumar, Malkeet
Okombo, John
Mambwe, Dickson
Taylor, Dale
Lawrence, Nina
Reader, Janette
van der Watt, Mariëtte
Fontinha, Diana
Sanches-Vaz, Margarida
Bezuidenhout, Belinda C.
Lauterbach, Sonja B.
Liebenberg, Dale
Birkholtz, Lyn-Marie
Coetzer, Theresa L.
Prudêncio, Miguel
Egan, Timothy J.
Wittlin, Sergio
Chibale, Kelly

January 2018

Astemizole analogues with reduced hERG inhibition as potent antimalarial compounds

Tian, Junjun
Vandermosten, Leen
Peigneur, Steve
Moreels, Lien
Rozenski, Jef
Tytgat, Jan
Herdewijn, Piet
Van den Steen, Philippe
De Jonghe, Steven

December 2017

Astemizole is a H1-antagonist endowed with antimalarial activity, but has hERG liabilities. Systemat...

Multistage Antiplasmodium Activity of Astemizole Analogues and Inhibition of Hemozoin Formation as a Contributor to Their Mode of Action

Malkeet Kumar (3104340)
John Okombo (561448)
Dickson Mambwe (6179453)
Dale Taylor (1463830)
Nina Lawrence (1463851)
Janette Reader (1484494)
Mariëtte van der Watt (6116213)
Diana Fontinha (589465)
Margarida Sanches-Vaz (6116210)
Belinda C. Bezuidenhout (6179456)
Sonja B. Lauterbach (6179459)
Dale Liebenberg (6179462)
Lyn-Marie Birkholtz (1484512)
Theresa L. Coetzer (269817)
Miguel Prudêncio (1434970)
Timothy J. Egan (262760)
Sergio Wittlin (181945)
Kelly Chibale (503778)

January 2019

A drug repositioning approach was leveraged to derivatize astemizole (AST), an antihistamine drug wh...

Structure-activity relationship studies and Plasmodium life cycle profiling identifies pan-active N-aryl-3-trifluoromethyl pyrido[1,2-a]benzimidazoles which are efficacious in an in vivo mouse model of malaria

Mayoka, Godfrey
Njoroge, Mathew
Okombo, John
Gibhard, Liezl
Sanches-Vaz, Margarida
Fontinha, Diana
Birkholtz, Lyn-Marie
Reader, Janette
Van der Watt, Mariette Elizabeth
Coetzer, Theresa L.
Lauterbach, Sonja B.
Churchyard, Alisje
Bezuidenhout, Belinda C.
Egan, Timothy J.
Yeates, Clive Leonard
Wittlin, Sergio
Prudêncio, Miguel
Chibale, Kelly

January 2019

Structure–activity relationship studies involving N-aryl-3-trifluoromethyl pyrido[1,2-a]benzimidazol...

Aminoindoles, a novel scaffold with potent activity against Plasmodium falciparum

Barker, R. H. Jr.
Urgaonkar, S.
Mazitschek, R.
Celatka, C.
Skerlj, R.
Cortese, J. F.
Tyndall, E.
Liu, H.
Cromwell, M.
Sidhu, A. B.
Guerrero-Bravo, J. E.
Crespo-Llado, K. N.
Serrano, A. E.
Lin, J. W.
Janse, C. J.
Khan, S. M.
Duraisingh, M.
Coleman, B. I.
Angulo-Barturen, I.
Jimenez-Diaz, M. B.
Magan, N.
Gomez, V.
Ferrer, S.
Martinez, M. S.
Wittlin, S.
Papastogiannidis, P.
O'Shea, T.
Klinger, J. D.
Bree, M.
Lee, E.
Levine, M.
Wiegand, R. C.
Munoz, B.
Wirth, D. F.
Clardy, J.
Bathurst, I.
Sybertz, E.

January 2011

This study characterizes aminoindole molecules that are analogs of Genz-644442. Genz-644442 was iden...

Exploring the transmission-blocking activity of antiplasmodial 3,6-diarylated imidazopyridazines

Coertzen, Dina
Reader, Janette
Van der Watt, Mariette Elizabeth
Leshabane, Meta Kgaogelo
Langeveld, Henrico
Cheuka, Peter M.
Dziwornu, Godwin Akpeko
Chibale, Kelly
Birkholtz, Lyn-Marie

January 2021

The effectiveness of current antimalarial therapies that cure patients of the pathogenic asexual blo...

Improvement of Asparagine Ethylenediamines as Anti-malarial

Zhan, Wenhu
Visone, Joseph
Ouellette, Tierra
Harris, Jacob C.
Wang, Rong
Zhang, Hao
Singh, Pradeep K.
Ginn, John
Sukenick, George
Wong, Tzu-Tshin
Okoro, Judith I
Scales, Ryan M
Tumwebaze, Patrick K
Rosenthal, Philip J
Kafsack, Björn F. C.
Cooper, Roland A.
Meinke, Peter T.
Kirkman, Laura A.
Lin, Gang

July 2019

The Plasmodium proteasome (Pf20S) emerged as a target for antimalarials. Pf20S inhibitors are active...

Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion

Nguyen, W.
Dans, M.G.
Ngo, A.
Gancheva, M.R.
Romeo, O.
Duffy, S.
de Koning-Ward, T.F.
Lowes, K.N.
Sabroux, H.J.
Avery, V.M.
Wilson, D.W.
Gilson, P.R.
Sleebs, B.E.

January 2021

The emerging resistance to combination therapies comprised of artemisinin derivatives has driven a n...

Chemical genetics of Plasmodium falciparum.

Guiguemde, W Armand
Shelat, Anang A
Bouck, David
Duffy, Sandra
Crowther, Gregory J
Davis, Paul H
Smithson, David C
Connelly, Michele
Clark, Julie
Zhu, Fangyi
Jiménez-Díaz, María B
Martinez, María S
Wilson, Emily B
Tripathi, Abhai K
Gut, Jiri
Sharlow, Elizabeth R
Bathurst, Ian
El Mazouni, Farah
Fowble, Joseph W
Forquer, Isaac
McGinley, Paula L
Castro, Steve
Angulo-Barturen, Iñigo
Ferrer, Santiago
Rosenthal, Philip J
Derisi, Joseph L
Sullivan, David J
Lazo, John S
Roos, David S
Riscoe, Michael K
Phillips, Margaret A
Rathod, Pradipsinh K
Van Voorhis, Wesley C
Avery, Vicky M
Guy, R Kiplin

May 2010

Malaria caused by Plasmodium falciparum is a disease that is responsible for 880,000 deaths per year...

Discovery and Structure−Activity Relationships of Pyrrolone

Dinakaran Murugesan
Alka Mital
Marcel Kaiser
David M. Shackleford
Julia Morizzi
Kasiram Katneni
Michael Campbell
Alan Hudson
Susan A. Charman
Clive Yeates
Ian H. Gilbert
Inpharma Consultancy

August 2016

*S Supporting Information ABSTRACT: In the pursuit of new antimalarial leads, a phenotypic screening...

Discovery of compounds blocking the proliferation of Toxoplasma gondii and Plasmodium falciparum in a chemical space based on piperidinyl-benzimidazolidinone analogs.

Saïdani, Nadia
Botté, Cyrille y
Deligny, Michael
Bonneau, Anne-Laure
Reader, Janette
Lasselin, Ronald
Merer, Goulven
Niepceron, Alisson
Brossier, Fabien
Cintrat, Jean-Christophe
Rousseau, Bernard
Birkholtz, Lyn-Marie
Cesbron-Delauw, Marie-France
Dubremetz, Jean-François
Mercier, Corinne
Vial, Henri
Lopez, Roman
Maréchal, Eric

February 2014

International audience: A piperidinyl-benzimidazolidinone scaffold has been found in the structure o...

RESEARCH ARTICLE Screening the Medicines for Malaria Venture "Malaria Box " against the Plasmodium

Falciparum Aminopeptidases
Ro Paiardini
Rebecca S. Bamert
Komagal Kannan-sivaraman
Nyssa Drinkwater
Shailesh N. Mistry
Peter J. Scammells
Sheena Mcgowan

August 2016

Malaria is a parasitic disease that remains a global health burden. The ability of the parasite to r...

Structure-Activity Relationships of Antiplasmodial Pantothenamide Analogues Reveal a New Way by Which Triazoles Mimic Amide Bonds

Guan, Jinming
Tjhin, Erick
Howieson, Vanessa
Kittikool, Tanakorn
Spry, Christina
Saliba, Kevin
Auclair, Karine

March 2019

Pantothenamides are potent growth inhibitors of the malaria parasite Plasmodium falciparum. Their cl...

New active drugs against liver stages of Plasmodium predicted by molecular topology.

Mahmoudi, N.
Garcia-Domenech, R.
Galvez, J.
Farhati, K.
Franetich, J.F.
Sauerwein, R.W.
Hannoun, L.
Derouin, F.
Danis, M.
Mazier, D.

January 2008

Item does not contain fulltextWe conducted a quantitative structure-activity relationship (QSAR) stu...

Antimalarial agents against both sexual and asexual parasites stages: structure-activity relationships and biological studies of the Malaria Box compound 1-[5-(4-bromo-2-chlorophenyl)furan-2-yl]-N-[(piperidin-4-yl)methyl]methanamine (MMV019918) and analogues

A. Vallone
S. D&apos
S. Brogi
M. Brindisi
G. Chemi
G. Alfano
S. Lamponi
S.G. Lee
J.M. Jez
K.J.M. Koolen
K.J. Dechering
S. Saponara
F. Fusi
B. Gorelli
D. Taramelli
S. Parapini
R. Caldelari
G. Campiani
S. Gemma
S. Butini

March 2018

Therapies addressing multiple stages of Plasmodium falciparum life cycle are highly desirable for im...

Multistage antiplasmodium activity of astemizole analogues and inhibition of hemozoin formation as a contributor to their mode of action

Kumar, Malkeet
Okombo, John
Mambwe, Dickson
Taylor, Dale
Lawrence, Nina
Reader, Janette
van der Watt, Mariëtte
Fontinha, Diana
Sanches-Vaz, Margarida
Bezuidenhout, Belinda C.
Lauterbach, Sonja B.
Liebenberg, Dale
Birkholtz, Lyn-Marie
Coetzer, Theresa L.
Prudêncio, Miguel
Egan, Timothy J.
Wittlin, Sergio
Chibale, Kelly

January 2018

Astemizole analogues with reduced hERG inhibition as potent antimalarial compounds

Tian, Junjun
Vandermosten, Leen
Peigneur, Steve
Moreels, Lien
Rozenski, Jef
Tytgat, Jan
Herdewijn, Piet
Van den Steen, Philippe
De Jonghe, Steven

December 2017

Astemizole is a H1-antagonist endowed with antimalarial activity, but has hERG liabilities. Systemat...

Multistage Antiplasmodium Activity of Astemizole Analogues and Inhibition of Hemozoin Formation as a Contributor to Their Mode of Action

Malkeet Kumar (3104340)
John Okombo (561448)
Dickson Mambwe (6179453)
Dale Taylor (1463830)
Nina Lawrence (1463851)
Janette Reader (1484494)
Mariëtte van der Watt (6116213)
Diana Fontinha (589465)
Margarida Sanches-Vaz (6116210)
Belinda C. Bezuidenhout (6179456)
Sonja B. Lauterbach (6179459)
Dale Liebenberg (6179462)
Lyn-Marie Birkholtz (1484512)
Theresa L. Coetzer (269817)
Miguel Prudêncio (1434970)
Timothy J. Egan (262760)
Sergio Wittlin (181945)
Kelly Chibale (503778)

January 2019

A drug repositioning approach was leveraged to derivatize astemizole (AST), an antihistamine drug wh...

Structure-activity relationship studies and Plasmodium life cycle profiling identifies pan-active N-aryl-3-trifluoromethyl pyrido[1,2-a]benzimidazoles which are efficacious in an in vivo mouse model of malaria

Mayoka, Godfrey
Njoroge, Mathew
Okombo, John
Gibhard, Liezl
Sanches-Vaz, Margarida
Fontinha, Diana
Birkholtz, Lyn-Marie
Reader, Janette
Van der Watt, Mariette Elizabeth
Coetzer, Theresa L.
Lauterbach, Sonja B.
Churchyard, Alisje
Bezuidenhout, Belinda C.
Egan, Timothy J.
Yeates, Clive Leonard
Wittlin, Sergio
Prudêncio, Miguel
Chibale, Kelly

January 2019

Structure–activity relationship studies involving N-aryl-3-trifluoromethyl pyrido[1,2-a]benzimidazol...

Aminoindoles, a novel scaffold with potent activity against Plasmodium falciparum

Barker, R. H. Jr.
Urgaonkar, S.
Mazitschek, R.
Celatka, C.
Skerlj, R.
Cortese, J. F.
Tyndall, E.
Liu, H.
Cromwell, M.
Sidhu, A. B.
Guerrero-Bravo, J. E.
Crespo-Llado, K. N.
Serrano, A. E.
Lin, J. W.
Janse, C. J.
Khan, S. M.
Duraisingh, M.
Coleman, B. I.
Angulo-Barturen, I.
Jimenez-Diaz, M. B.
Magan, N.
Gomez, V.
Ferrer, S.
Martinez, M. S.
Wittlin, S.
Papastogiannidis, P.
O'Shea, T.
Klinger, J. D.
Bree, M.
Lee, E.
Levine, M.
Wiegand, R. C.
Munoz, B.
Wirth, D. F.
Clardy, J.
Bathurst, I.
Sybertz, E.

January 2011

This study characterizes aminoindole molecules that are analogs of Genz-644442. Genz-644442 was iden...

Exploring the transmission-blocking activity of antiplasmodial 3,6-diarylated imidazopyridazines

Coertzen, Dina
Reader, Janette
Van der Watt, Mariette Elizabeth
Leshabane, Meta Kgaogelo
Langeveld, Henrico
Cheuka, Peter M.
Dziwornu, Godwin Akpeko
Chibale, Kelly
Birkholtz, Lyn-Marie

January 2021

The effectiveness of current antimalarial therapies that cure patients of the pathogenic asexual blo...

Improvement of Asparagine Ethylenediamines as Anti-malarial

Zhan, Wenhu
Visone, Joseph
Ouellette, Tierra
Harris, Jacob C.
Wang, Rong
Zhang, Hao
Singh, Pradeep K.
Ginn, John
Sukenick, George
Wong, Tzu-Tshin
Okoro, Judith I
Scales, Ryan M
Tumwebaze, Patrick K
Rosenthal, Philip J
Kafsack, Björn F. C.
Cooper, Roland A.
Meinke, Peter T.
Kirkman, Laura A.
Lin, Gang

July 2019

The Plasmodium proteasome (Pf20S) emerged as a target for antimalarials. Pf20S inhibitors are active...

Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion

Nguyen, W.
Dans, M.G.
Ngo, A.
Gancheva, M.R.
Romeo, O.
Duffy, S.
de Koning-Ward, T.F.
Lowes, K.N.
Sabroux, H.J.
Avery, V.M.
Wilson, D.W.
Gilson, P.R.
Sleebs, B.E.

January 2021

The emerging resistance to combination therapies comprised of artemisinin derivatives has driven a n...

Chemical genetics of Plasmodium falciparum.

Guiguemde, W Armand
Shelat, Anang A
Bouck, David
Duffy, Sandra
Crowther, Gregory J
Davis, Paul H
Smithson, David C
Connelly, Michele
Clark, Julie
Zhu, Fangyi
Jiménez-Díaz, María B
Martinez, María S
Wilson, Emily B
Tripathi, Abhai K
Gut, Jiri
Sharlow, Elizabeth R
Bathurst, Ian
El Mazouni, Farah
Fowble, Joseph W
Forquer, Isaac
McGinley, Paula L
Castro, Steve
Angulo-Barturen, Iñigo
Ferrer, Santiago
Rosenthal, Philip J
Derisi, Joseph L
Sullivan, David J
Lazo, John S
Roos, David S
Riscoe, Michael K
Phillips, Margaret A
Rathod, Pradipsinh K
Van Voorhis, Wesley C
Avery, Vicky M
Guy, R Kiplin

May 2010

Malaria caused by Plasmodium falciparum is a disease that is responsible for 880,000 deaths per year...

Discovery and Structure−Activity Relationships of Pyrrolone

Dinakaran Murugesan
Alka Mital
Marcel Kaiser
David M. Shackleford
Julia Morizzi
Kasiram Katneni
Michael Campbell
Alan Hudson
Susan A. Charman
Clive Yeates
Ian H. Gilbert
Inpharma Consultancy

August 2016

*S Supporting Information ABSTRACT: In the pursuit of new antimalarial leads, a phenotypic screening...

Discovery of compounds blocking the proliferation of Toxoplasma gondii and Plasmodium falciparum in a chemical space based on piperidinyl-benzimidazolidinone analogs.

Saïdani, Nadia
Botté, Cyrille y
Deligny, Michael
Bonneau, Anne-Laure
Reader, Janette
Lasselin, Ronald
Merer, Goulven
Niepceron, Alisson
Brossier, Fabien
Cintrat, Jean-Christophe
Rousseau, Bernard
Birkholtz, Lyn-Marie
Cesbron-Delauw, Marie-France
Dubremetz, Jean-François
Mercier, Corinne
Vial, Henri
Lopez, Roman
Maréchal, Eric

February 2014

International audience: A piperidinyl-benzimidazolidinone scaffold has been found in the structure o...

RESEARCH ARTICLE Screening the Medicines for Malaria Venture "Malaria Box " against the Plasmodium

Falciparum Aminopeptidases
Ro Paiardini
Rebecca S. Bamert
Komagal Kannan-sivaraman
Nyssa Drinkwater
Shailesh N. Mistry
Peter J. Scammells
Sheena Mcgowan

August 2016

Malaria is a parasitic disease that remains a global health burden. The ability of the parasite to r...

Structure-Activity Relationships of Antiplasmodial Pantothenamide Analogues Reveal a New Way by Which Triazoles Mimic Amide Bonds

Guan, Jinming
Tjhin, Erick
Howieson, Vanessa
Kittikool, Tanakorn
Spry, Christina
Saliba, Kevin
Auclair, Karine

March 2019

Pantothenamides are potent growth inhibitors of the malaria parasite Plasmodium falciparum. Their cl...

New active drugs against liver stages of Plasmodium predicted by molecular topology.

Mahmoudi, N.
Garcia-Domenech, R.
Galvez, J.
Farhati, K.
Franetich, J.F.
Sauerwein, R.W.
Hannoun, L.
Derouin, F.
Danis, M.
Mazier, D.

January 2008

Item does not contain fulltextWe conducted a quantitative structure-activity relationship (QSAR) stu...

Antimalarial agents against both sexual and asexual parasites stages: structure-activity relationships and biological studies of the Malaria Box compound 1-[5-(4-bromo-2-chlorophenyl)furan-2-yl]-N-[(piperidin-4-yl)methyl]methanamine (MMV019918) and analogues

A. Vallone
S. D&apos
S. Brogi
M. Brindisi
G. Chemi
G. Alfano
S. Lamponi
S.G. Lee
J.M. Jez
K.J.M. Koolen
K.J. Dechering
S. Saponara
F. Fusi
B. Gorelli
D. Taramelli
S. Parapini
R. Caldelari
G. Campiani
S. Gemma
S. Butini

March 2018

Therapies addressing multiple stages of Plasmodium falciparum life cycle are highly desirable for im...

Structure−activity relationship studies reveal new astemizole analogues active against Plasmodium falciparum in vitro

Abstract

Extracted data

Structure−activity relationship studies reveal new astemizole analogues active against Plasmodium falciparum in vitro

Abstract

Extracted data

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