Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Josefina Santo-Tomas"'
Autor:
Josefina Santo Tomas, Christopher Snyder, Jessica Anne Steuten, Sergio Wittlin, Francis C. K. Chiu, Jacques Chollet, Xiaofang Wang, Kasiram Katneni, Yuxiang Dong, Eileen Ryan, Jonathan L. Vennerstrom, Susan A. Charman, Christian Scheurer, Julia Morizzi, Janne Mannila
Publikováno v:
Journal of Medicinal Chemistry. 56:2547-2555
To ascertain the structure–activity relationship of the core 1,2,4-trioxolane substructure of dispiro ozonides OZ277 and OZ439, we compared the antimalarial activities and ADME profiles of the 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::42ce32fde6bd7958f4aa225afbff7e39
https://doi.org/10.1021/jm400004u
https://doi.org/10.1021/jm400004u
Autor:
Christopher Snyder, Hugues Matile, Jacques Chollet, Francis C. K. Chiu, Arnulf Dorn, Yuxiang Dong, Heinrich Urwyler, Yuanqing Tang, Julia Morizzi, Susan A. Charman, William N. Charman, Lisa M. Johnson, Jonathan L. Vennerstrom, Sergio Wittlin, Josefina Santo Tomas, Lin Zhou, Christian Scheurer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:563-566
Thirty-three N-acyl 1,2,4-dispiro trioxolanes (secondary ozonides) were synthesized. For these ozonides, weak base functional groups were not required for high antimalarial potency against Plasmodium falciparum in vitro, but were necessary for high a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a44dea2ddde727bcd37a6def0e4b20cf
https://doi.org/10.1016/j.bmcl.2009.11.088
https://doi.org/10.1016/j.bmcl.2009.11.088
Autor:
Jonathan L. Vennerstrom, Heinrich Urwyler, Sergio Wittlin, Yuxiang Dong, Darren J. Creek, Yuanqing Tang, Arnulf Dorn, Kamaraj Sriraghavan, Christopher Snyder, Julia Morizzi, Reto Brun, Maniyan Padmanilayam, Maria Koltun, Susan A. Charman, William N. Charman, Jacques Chollet, Xiaofang Wang, Hugues Matile, Josefina Santo Tomas, Christian Scheurer
Publikováno v:
Journal of Medicinal Chemistry. 53:481-491
The structure and stereochemistry of the cyclohexane substituents of analogues of arterolane (OZ277) had little effect on potency against Plasmodium falciparum in vitro. Weak base functional groups were not required for high antimalarial potency, but
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::597e9be51453d7021377a69512c5262a
https://doi.org/10.1021/jm901473s
https://doi.org/10.1021/jm901473s
Autor:
Remo Stohler, Reto Brun, Lindsey Catherine Hess, Sandra Sinishtaj, Alvin S. Kalinda, Aimee R. Usera, Kimberly S. Petersen, John G. D'angelo, Gary H. Posner, Theresa A. Shapiro, Andrew S. Rosenthal, Josefina Santo-Tomas, William A. Maio, Christopher Snyder, Sergio Wittlin, Jacques Chollet, Matthias Rottmann, Lauren E. Woodard, Wonsuk Chang
Publikováno v:
Journal of Medicinal Chemistry. 51:1035-1042
In four or five chemical steps from the 1,2,4-trioxane artemisinin, a new series of 23 trioxane dimers has been prepared. Eleven of these new trioxane dimers cure malaria-infected mice via oral dosing at 3 x 30 mg/kg. The clinically used trioxane dru
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78e16abd7fbd9eace1ec0df664837f2f
https://doi.org/10.1021/jm701168h
https://doi.org/10.1021/jm701168h
Autor:
Sergio Wittlin, Christopher Snyder, Christian Scheurer, Josefina Santo-Tomas, Jacques Chollet
Publikováno v:
Experimental Parasitology. 115:296-300
RBx11160 (OZ277) is a promising antimalarial drug candidate that Ranbaxy Laboratories Limited and Medicines for Malaria Venture (MMV) are currently developing as a fixed combination with piperaquine. Here, we describe the in vitro (Plasmodium falcipa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c6ce09f12c414cd32a326e0b0f2d93cf
https://doi.org/10.1016/j.exppara.2006.09.016
https://doi.org/10.1016/j.exppara.2006.09.016
Autor:
Jonathan L. Vennerstrom, Darren J. Creek, Bernard Scorneaux, Sergio Wittlin, Josefina Santo Tomas, Hugues Matile, Christian Scheurer, Maniyan Padmanilayam, Reto Brun, Jacques Chollet, William N. Charman, Susan A. Charman, Yuxiang Dong
Publikováno v:
Monash University
With an aim to identify a dispiro-1,2,4-trioxolane with high oral activity and good physicochemical properties, 27 derivatives of an achiral piperidine trioxolane were synthesized; most were potent antimalarial peroxides with IC(50)s ranging from 0.2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87d71fcde0df6ae1677852037b279733
https://doi.org/10.1016/j.bmcl.2006.08.046
https://doi.org/10.1016/j.bmcl.2006.08.046
Autor:
Scott A Alexander, Jonathan L. Vennerstrom, Saroj Bajpai, William N. Charman, Christopher Snyder, Christian Scheurer, Maniyan Padmanilayam, Josefina Santo Tomas, Yuanqing Tang, Sergio Wittlin, Hugues Matile, Bernard Scorneaux, Yuxiang Dong, Susan A. Charman, Jacques Chollet, Xiaofang Wang, Srinivasa Rao Cheruku, Reto Brun
Publikováno v:
Bioorganic & Medicinal Chemistry. 14:6368-6382
Based on the structures of several lipophilic trioxolane antimalarial prototypes, we set out to determine which functional groups were associated with good antimalarial profiles and identify more polar (lower LogP/LogD) lead compounds with good physi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8a8ad2a5b6995fb17698f245bffad38c
https://doi.org/10.1016/j.bmc.2006.05.041
https://doi.org/10.1016/j.bmc.2006.05.041
Autor:
Sergio Wittlin, Josefina Santo Tomas, Jonathan L. Vennerstrom, Jacques Chollet, Xiaofang Wang, Darren J. Creek, Yuxiang Dong, Christopher Snyder, Susan A. Charman, Christian Scheurer
Publikováno v:
Journal of medicinal chemistry. 50(23)
Fourteen spiro- and dispiro-1,2-dioxolanes were synthesized by peroxycarbenium ion annulations with alkenes in yields ranging from 30% to 94%. Peroxycarbenium ion precursors included triethylsilyldiperoxyketals and -acetals derived from geminal dihyd
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::21f05779c2eb3a2122d8e688d898b649
https://pubmed.ncbi.nlm.nih.gov/17949067
https://pubmed.ncbi.nlm.nih.gov/17949067
Autor:
William N. Charman, Jacques Chollet, Xiaofang Wang, Hugues Matile, Reto Brun, Susan A. Charman, Jonathan L. Vennerstrom, Christian Scheurer, Bernard Scorneaux, Josefina Santo Tomas, Yuanqing Tang, Arnulf Dorn, Heinrich Urwyler, Yuxiang Dong, Jean M. Karle, Christopher Snyder, Francis C. K. Chiu, Sergio Wittlin
Publikováno v:
Journal of medicinal chemistry. 48(15)
This paper describes the discovery of synthetic 1,2,4-trioxolane antimalarials and how we established a workable structure-activity relationship in the context of physicochemical, biopharmaceutical, and toxicological profiling. An achiral dispiro-1,2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b4b58650b675a9b4ca9667244c923691
https://pubmed.ncbi.nlm.nih.gov/16033274
https://pubmed.ncbi.nlm.nih.gov/16033274
Autor:
William N. Charman, Jonathan L. Vennerstrom, Susan A. Charman, Jacques Chollet, Josefina Santo Tomas, Kylie Anne McIntosh, Yuanqing Tang, Hugues Matile, Yuxiang Dong, Maniyan Padmanilayam, Daniel Hunziker, Sergio Wittlin, Bernard Scorneaux, Sarah Arbe-Barnes, Reto Brun, Heinrich Urwyler, Francis C. K. Chiu, Christian Scheurer, Arnulf Dorn
Publikováno v:
Nature. 430(7002)
The discovery of artemisinin more than 30 years ago provided a completely new antimalarial structural prototype; that is, a molecule with a pharmacophoric peroxide bond in a unique 1,2,4-trioxane heterocycle. Available evidence suggests that artemisi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::270642be1357eebb33067ddf6cbae260
https://pubmed.ncbi.nlm.nih.gov/15318201
https://pubmed.ncbi.nlm.nih.gov/15318201