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Volumn 54, Issue 18, 2011, Pages 6277-6285

Structure-activity relationships of 4-position diamine quinoline methanols as intermittent preventative treatment (IPT) against plasmodium falciparum

Author keywords

[No Author keywords available]

Indexed keywords

1 [2,8 BIS(TRIFLUOROMETHYL)QUINOLIN 4 YL] 2 [2 (CYCLOPROPYLAMINO)ETHYLAMINO]ETHANOL; ANTIMALARIAL AGENT; MEFLOQUINE; UNCLASSIFIED DRUG; WR 621308;

EID: 80052786962     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm200647u     Document Type: Article
Times cited : (21)

References (16)
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    • Dow, G. S.; Magill, A. J.; Ohrt, C. Clinical development of new prophylactic antimalarial drugs after the 5th Amendment to the Declaration of Helsinki Ther. Clin. Risk Manage. 2008, 4
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    • Dow, G.S.1    Magill, A.J.2    Ohrt, C.3
  • 2
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    • Intermittent treatment for the prevention of malaria during pregnancy in Benin: A randomized, open-label equivalence trial comparing sulfadoxine- pyrimethamine with mefloquine
    • Briand, V.; Bottero, J; Noël, H.; Masse, V.; Cordel, H.; Guerra, J.; Kossou, H.; Fayomi, B.; Ayemonna, P.; Fievet, N.; Massougbodji, A.; Cot, M. Intermittent treatment for the prevention of malaria during pregnancy in Benin: a randomized, open-label equivalence trial comparing sulfadoxine-pyrimethamine with mefloquine J. Infect. Dis. 2009, 200, 991-1001
    • (2009) J. Infect. Dis. , vol.200 , pp. 991-1001
    • Briand, V.1    Bottero, J.2    Noël, H.3    Masse, V.4    Cordel, H.5    Guerra, J.6    Kossou, H.7    Fayomi, B.8    Ayemonna, P.9    Fievet, N.10    Massougbodji, A.11    Cot, M.12
  • 3
    • 77953799477 scopus 로고    scopus 로고
    • Intermittent preventive treatment of infants with mefloquine reduces risk of clinical malaria in areas of moderate malaria transmission and high resistance to sulphadoxine-pyrimethamine, but safety and tolerability issues need consideration
    • McGready, R. Intermittent preventive treatment of infants with mefloquine reduces risk of clinical malaria in areas of moderate malaria transmission and high resistance to sulphadoxine-pyrimethamine, but safety and tolerability issues need consideration Evidence-Based Med. 2010, 15, 71-72
    • (2010) Evidence-Based Med. , vol.15 , pp. 71-72
    • McGready, R.1
  • 7
    • 70349802009 scopus 로고    scopus 로고
    • Synthesis and biological evaluation of the first pentafluorosulfanyl analogs of mefloquine
    • Wipf, P.; Mo, T.; Geib, S.; Caridha, D.; Dow, G.; Gerena, L.; Roncal, N.; Milner, E. Synthesis and biological evaluation of the first pentafluorosulfanyl analogs of mefloquine Org. Biomol. Chem. 2009, 7, 4163-4165
    • (2009) Org. Biomol. Chem. , vol.7 , pp. 4163-4165
    • Wipf, P.1    Mo, T.2    Geib, S.3    Caridha, D.4    Dow, G.5    Gerena, L.6    Roncal, N.7    Milner, E.8
  • 8
    • 77956225873 scopus 로고    scopus 로고
    • Synthesis of 8-pentafluorosulfanyl analog of the antimalarial agent mefloquine
    • Mo, T.; Milner, E.; Dow, G.; Wipf, P. Synthesis of 8-pentafluorosulfanyl analog of the antimalarial agent mefloquine Tetrahedron Lett. 2010, 51, 5137-5140
    • (2010) Tetrahedron Lett. , vol.51 , pp. 5137-5140
    • Mo, T.1    Milner, E.2    Dow, G.3    Wipf, P.4
  • 9
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    • Initially (+)- and (-)-enantiomers of epoxide 3 were obtained via supercritical fluid chromatographic separation performed by Regis Technology (; refer to Supporting Information for chromatogram). Once a lead candidate was declared, the bulk synthesis of the corresponding (+) enantiomer of epoxide 3 was out-sourced to Bioblocks (http://www.bioblocks.com).
    • Initially (+)- and (-)-enantiomers of epoxide 3 were obtained via supercritical fluid chromatographic separation performed by Regis Technology (http://www.registech.com; refer to Supporting Information for chromatogram). Once a lead candidate was declared, the bulk synthesis of the corresponding (+) enantiomer of epoxide 3 was out-sourced to Bioblocks (http://www.bioblocks.com).
  • 13
    • 80052786356 scopus 로고    scopus 로고
    • United States Food and Drug Administration, Center for Drug Evaluation and Research. United States Department of Health and Human Services: Washington, DC.
    • United States Food and Drug Administration, Center for Drug Evaluation and Research. Development of New Stereoisomeric Drugs; United States Department of Health and Human Services: Washington, DC, 2005; http://www.fda.gov/Drugs/ GuidanceComplianceRegulatoryInformation/Guidances/.
    • (2005) Development of New Stereoisomeric Drugs
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    • United States Food and Drug Administration, Center for Drug Evaluation and Research. United States Department of Health and Human Services: Washington, DC
    • United States Food and Drug Administration, Center for Drug Evaluation and Research. Guidance for Industry: Estimating the Maximum Safe Starting Dose in Initial Clinical Trials for Therapeutics in Healthy Volunteers; United States Department of Health and Human Services: Washington, DC, 2005; http://www.fda.gov/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/
    • (2005) Guidance for Industry: Estimating the Maximum Safe Starting Dose in Initial Clinical Trials for Therapeutics in Healthy Volunteers
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    • The tables in the article were developed using SAR Vision software, info@chemapps.com.
    • The tables in the article were developed using SAR Vision software, info@chemapps.com.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.