The use of a prodrug approach to minimize potential CNS exposure of next generation quinoline methanols while maintaining efficacy in in vivo animal models

European Journal of Drug Metabolism and Pharmacokinetics

Volumn 39, Issue 4, 2014, Pages 231-236

  Sousa, Jason C ^a   Milner, Erin ^a   Carroll, Dustin ^a   McCalmont, William ^a   Gardner, Sean ^a   Moon, Jay ^a   Johnson, Jacob D ^a   Lee, Patricia ^a   Auschwitz, Jennifer ^a   Roncal, Norma ^a   Caridha, Diana ^a   Tungteung, Anchalee ^b   Zeng, Qiang ^a   Reyes, Sean ^a   Smith, Bryan ^a   Li, Qigui ^a   Kozar, Michael P ^a   Melendez, Victor ^a   Dow, Geoffrey ^a,b  

^a WALTER REED ARMY INSTITUTE OF RESEARCH   (United States)

^b U S ARMY   (United States)

Author keywords

Blood brain barrier; Central nervous system; Malaria; Mefloquine; Prodrug; Quinoline methanol

Indexed keywords

ANTIMALARIAL AGENT; MEFLOQUINE; PRODRUG; WR319670;

ANALOGS AND DERIVATIVES; ANIMAL; BLOOD BRAIN BARRIER; INSTITUTE FOR CANCER RESEARCH MOUSE; MALE; MOUSE;

ANIMALS; ANTIMALARIALS; BLOOD-BRAIN BARRIER; MALE; MEFLOQUINE; MICE; MICE, INBRED ICR; PRODRUGS;

EID: 84897357409     PISSN: 03787966     EISSN: 21070180     Source Type: Journal    
DOI: 10.1007/s13318-013-0162-9     Document Type: Article

References (14)

1. Arguin PM, Mali S (2012) Malaria. CDC Yellow Book. http://wwwnc.cdc.gov/travel/yellowbook/2012/chapter-3-infectious-diseases-related-to-travel/malaria.htm. Accessed 12 Dec 2012
2. Caridha D, Yourick D, Cabezas M, Wolf L, Hudson TH, Dow GS (2008) Mefloquine-induced disruption of calcium homeostasis in mammalian cells is similar to that induced by ionomycin. Antimicrob Agents Chemother 52:684-693
3. Chulay JD, Haynes JD, Diggs CL (1983) Plasmodium falciparum - assessment of in vitro growth by [H-3]-labeled hypoxanthine incorporation. Exp Parasitol 55:138-146
4. Chung MC, Ferreira EI et al (2008) Prodrugs for the treatment of neglected diseases. Molecules 13:616-677
5. Desjardins RE, Canfield CJ, Haynes JD, Chulay JD (1979) Quantitative assessment of antimalarial activity in vitro by a semiautomated microdilution technique. Antimicrob Agents Chemother 16:710-718
6. Dow GS, Heady TN et al (2006) Utility of alkylaminoquinolinyl methanols as new antimalarial drugs. Antimicrob Agents Chemother 50:4132-4143
7. Dow GS, Magill AJ, Ohrt C (2008) Clinical development of new prophylactic antimalarial drugs after the 5th Amendment to the Declaration of Helsinki. Ther Clin Risk Manag 4:803-819
8. Johnson JD, Dennull RA, Gerena L, Lopez-Sanchez M, Roncal NE, Waters NC (2007) Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening. Antimicrob Agents Chemother 51:1926-1933
9. Milhous WK, Weatherly NF, Bowdre JH, Desjardins RE (1985) In vitro activities of and mechanisms of resistance to antifol antimalarial drugs. Antimicrob Agents Chemother 27:525-530
10. Milner E, McCalmont W et al (2010a) Structure-activity relationships amongst 4-position quinoline methanol antimalarials that inhibit the growth of drug sensitive and resistant strains of Plasmodium falciparum. Bioorg Med Chem Lett 20:1347-1351
11. Milner E, McCalmont W et al (2010b) Anti-malarial activity of a non-piperidine library of next-generation quinoline methanols. Malar J 9:51-60
12. Smilkstein M, Sriwilaijaroen N, Kelly JX, Wilairat P, Riscoe M (2004) Simple and inexpensive fluorescence-based technique for high-throughput antimalarial drug screening. Antimicrob Agents Chemother 48:1803-1806
13. Toovey S (2009) Mefloquine neurotoxicity: a literature review. Travel Med Infect Dis 7:2-6
14. Yelmo S, Morera-Fumero AL, Henry M, Renshaw A, Gracia-Marco R (2010) Mania Associated With Mefloquine Prophylaxis. J Clin Psychopharmacol 30:339-341