New Chimeric Antimalarials with 4-Aminoquinoline Moiety Linked to a Tetraoxane Skeleton. Opsenica, I., Opsenica, D., Lanteri, C. A., Anova, L., Milhous, W. K., Smith, K. S., & Šolaja, B. A. J.~Med.~Chem., 51(19):6216--6219, 2008.
Paper abstract bibtex Abstract: The synthesis of the chimeric molecules consisting of two pharmacophores, tetraoxane and 7-chloro-4-aminoquinoline, is reported. The tetraoxanes 2, 4, and 8 show relatively potent in vitro antimalarial activities, with IC90 values for the Plasmodium falciparum strain W2 of 2.26, 12.44, and 10.74 nM, respectively. In addition, two compounds, 2 and 4, cured mice in a modified Thompson test for antimalarial blood stage activity, with a minimum curative dose of 80 mg/kg, a minimum active dose of 20 mg/kg/day, and a maximum tolerated dose of >960 mg/kg.
@article{Opsenica:2008aa,
Abstract = {Abstract: The synthesis of the chimeric molecules consisting of two pharmacophores, tetraoxane and 7-chloro-4-aminoquinoline, is reported. The tetraoxanes 2, 4, and 8 show relatively potent in vitro antimalarial activities, with IC90 values for the Plasmodium falciparum strain W2 of 2.26, 12.44, and 10.74 nM, respectively. In addition, two compounds, 2 and 4, cured mice in a modified Thompson test for antimalarial blood stage activity, with a minimum curative dose of 80 mg/kg, a minimum active dose of 20 mg/kg/day, and a maximum tolerated dose of >960 mg/kg.},
Author = {Opsenica, Igor and Opsenica, Dejan and Lanteri, Charlotte Anne and Anova, Lalaine and Milhous, Wilbur K. and Smith, Kirsten S. and S\&{\#}x30c;olaja, Bogdan A.},
Date-Added = {2008-09-29 14:14:01 -0400},
Date-Modified = {2009-04-06 22:32:49 -0400},
Journal = {J.~Med.~Chem.},
Keywords = {malaria; artemisinin; radical; heme; epoxide},
Number = {19},
Pages = {6216--6219},
Title = {New Chimeric Antimalarials with 4-Aminoquinoline Moiety Linked to a Tetraoxane Skeleton},
Url = {http://pubs3.acs.org/acs/journals/doilookup?in_doi=10.1021/jm8006905},
Volume = {51},
Year = {2008},
Bdsk-File-1 = {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},
Bdsk-Url-1 = {http://dx.doi.org/10.1021/jm8006905}}
Downloads: 0
{"_id":"22KBcPoJmWusXaTPq","bibbaseid":"opsenica-opsenica-lanteri-anova-milhous-smith-sx30colaja-newchimericantimalarialswith4aminoquinolinemoietylinkedtoatetraoxaneskeleton-2008","downloads":0,"creationDate":"2016-02-18T13:03:31.365Z","title":"New Chimeric Antimalarials with 4-Aminoquinoline Moiety Linked to a Tetraoxane Skeleton","author_short":["Opsenica, I.","Opsenica, D.","Lanteri, C. A.","Anova, L.","Milhous, W. K.","Smith, K. S.","Šolaja, B. A."],"year":2008,"bibtype":"article","biburl":"https://dl.dropboxusercontent.com/u/26998770/main.bib","bibdata":{"bibtype":"article","type":"article","abstract":"Abstract: The synthesis of the chimeric molecules consisting of two pharmacophores, tetraoxane and 7-chloro-4-aminoquinoline, is reported. The tetraoxanes 2, 4, and 8 show relatively potent in vitro antimalarial activities, with IC90 values for the Plasmodium falciparum strain W2 of 2.26, 12.44, and 10.74 nM, respectively. In addition, two compounds, 2 and 4, cured mice in a modified Thompson test for antimalarial blood stage activity, with a minimum curative dose of 80 mg/kg, a minimum active dose of 20 mg/kg/day, and a maximum tolerated dose of >960 mg/kg.","author":[{"propositions":[],"lastnames":["Opsenica"],"firstnames":["Igor"],"suffixes":[]},{"propositions":[],"lastnames":["Opsenica"],"firstnames":["Dejan"],"suffixes":[]},{"propositions":[],"lastnames":["Lanteri"],"firstnames":["Charlotte","Anne"],"suffixes":[]},{"propositions":[],"lastnames":["Anova"],"firstnames":["Lalaine"],"suffixes":[]},{"propositions":[],"lastnames":["Milhous"],"firstnames":["Wilbur","K."],"suffixes":[]},{"propositions":[],"lastnames":["Smith"],"firstnames":["Kirsten","S."],"suffixes":[]},{"propositions":[],"lastnames":["Šolaja"],"firstnames":["Bogdan","A."],"suffixes":[]}],"date-added":"2008-09-29 14:14:01 -0400","date-modified":"2009-04-06 22:32:49 -0400","journal":"J.~Med.~Chem.","keywords":"malaria; artemisinin; radical; heme; epoxide","number":"19","pages":"6216--6219","title":"New Chimeric Antimalarials with 4-Aminoquinoline Moiety Linked to a Tetraoxane Skeleton","url":"http://pubs3.acs.org/acs/journals/doilookup?in_doi=10.1021/jm8006905","volume":"51","year":"2008","bdsk-file-1":"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","bdsk-url-1":"http://dx.doi.org/10.1021/jm8006905","bibtex":"@article{Opsenica:2008aa,\n\tAbstract = {Abstract: The synthesis of the chimeric molecules consisting of two pharmacophores, tetraoxane and 7-chloro-4-aminoquinoline, is reported. The tetraoxanes 2, 4, and 8 show relatively potent in vitro antimalarial activities, with IC90 values for the Plasmodium falciparum strain W2 of 2.26, 12.44, and 10.74 nM, respectively. In addition, two compounds, 2 and 4, cured mice in a modified Thompson test for antimalarial blood stage activity, with a minimum curative dose of 80 mg/kg, a minimum active dose of 20 mg/kg/day, and a maximum tolerated dose of >960 mg/kg.},\n\tAuthor = {Opsenica, Igor and Opsenica, Dejan and Lanteri, Charlotte Anne and Anova, Lalaine and Milhous, Wilbur K. and Smith, Kirsten S. and S\\&{\\#}x30c;olaja, Bogdan A.},\n\tDate-Added = {2008-09-29 14:14:01 -0400},\n\tDate-Modified = {2009-04-06 22:32:49 -0400},\n\tJournal = {J.~Med.~Chem.},\n\tKeywords = {malaria; artemisinin; radical; heme; epoxide},\n\tNumber = {19},\n\tPages = {6216--6219},\n\tTitle = {New Chimeric Antimalarials with 4-Aminoquinoline Moiety Linked to a Tetraoxane Skeleton},\n\tUrl = {http://pubs3.acs.org/acs/journals/doilookup?in_doi=10.1021/jm8006905},\n\tVolume = {51},\n\tYear = {2008},\n\tBdsk-File-1 = {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},\n\tBdsk-Url-1 = {http://dx.doi.org/10.1021/jm8006905}}\n\n","author_short":["Opsenica, I.","Opsenica, D.","Lanteri, C. A.","Anova, L.","Milhous, W. K.","Smith, K. S.","Šolaja, B. A."],"key":"Opsenica:2008aa","id":"Opsenica:2008aa","bibbaseid":"opsenica-opsenica-lanteri-anova-milhous-smith-sx30colaja-newchimericantimalarialswith4aminoquinolinemoietylinkedtoatetraoxaneskeleton-2008","role":"author","urls":{"Paper":"http://pubs3.acs.org/acs/journals/doilookup?in_doi=10.1021/jm8006905"},"keyword":["malaria; artemisinin; radical; heme; epoxide"],"downloads":0},"search_terms":["new","chimeric","antimalarials","aminoquinoline","moiety","linked","tetraoxane","skeleton","opsenica","opsenica","lanteri","anova","milhous","smith","šolaja"],"keywords":["malaria; artemisinin; radical; heme; epoxide"],"authorIDs":[],"dataSources":["c5japf9eAQRaeMS4h"]}