{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,26]],"date-time":"2026-09-26T14:19:50Z","timestamp":1790432390220,"version":"4.1.0"},"reference-count":37,"publisher":"American Society for Microbiology","issue":"6","license":[{"start":{"date-parts":[[2012,6,1]],"date-time":"2012-06-01T00:00:00Z","timestamp":1338508800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.asm.org\/non-commercial-tdm-license"}],"content-domain":{"domain":["journals.asm.org"],"crossmark-restriction":true},"short-container-title":["Antimicrob Agents Chemother"],"published-print":{"date-parts":[[2012,6]]},"abstract":"<jats:title>ABSTRACT<\/jats:title>\n          <jats:p>\n            Interesting antischistosomal properties have been documented for the antimalarial mefloquine, a 4-quinolinemethanol. We evaluated the antischistosomal activities of nine mefloquine-related compounds belonging to the 4-pyridinemethanols, 9-phenanthrenmethanols, and 4-quinolinemethanols. Eight compounds revealed high activities against\n            <jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">Schistosoma mansoni in vitro<\/jats:named-content>\n            , with two drugs (the 4-quinolinemethanols WR7573 and WR7930) characterized by significantly lower half-maximal inhibitory concentrations (IC\n            <jats:sub>50<\/jats:sub>\n            s) (2.7 and 3.5 \u03bcM, respectively) compared to mefloquine (11.4 \u03bcM). Mefloquine and WR7930 showed significantly decreased IC\n            <jats:sub>50<\/jats:sub>\n            s when incubated in the presence of hemoglobin. High worm burden reductions (WBR) were obtained with enpiroline (WBR, 82.7%; dosage, 200 mg\/kg of body weight) and its\n            <jats:italic>threo<\/jats:italic>\n            isomers (+)-\n            <jats:italic>threo<\/jats:italic>\n            (WBR, 100%) and (\u2212)-\n            <jats:italic>threo<\/jats:italic>\n            (WBR, 89%) and with WR7930 (WBR, 87%; dosage, 100 mg\/kg) against adult\n            <jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">S. mansoni<\/jats:named-content>\n            in mice. Furthermore, excellent\n            <jats:italic>in vitro<\/jats:italic>\n            and\n            <jats:italic>in vivo<\/jats:italic>\n            antischistosomal activity was observed for two WR7930-related structures (WR29252 and WR7524). In addition, mefloquine (WBR, 81%), enpiroline (WBR, 77%), and WR7930 (WBR, 100%) showed high activities against\n            <jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">S. haematobium<\/jats:named-content>\n            harbored in mice following single oral doses of 200 mg\/kg. These results provide a deeper insight into the structural features of the arylmethanols that rule antischistosomal activity. Further studies should be launched with enpiroline and WR7930.\n          <\/jats:p>","DOI":"10.1128\/aac.06177-11","type":"journal-article","created":{"date-parts":[[2012,4,3]],"date-time":"2012-04-03T04:58:03Z","timestamp":1333429083000},"page":"3207-3215","update-policy":"https:\/\/doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":49,"title":["Antischistosomal Activities of Mefloquine-Related Arylmethanols"],"prefix":"10.1128","volume":"56","author":[{"given":"Katrin","family":"Ingram","sequence":"first","affiliation":[{"name":"Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Basel, Switzerland"},{"name":"University of Basel, Basel, Switzerland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"William","family":"Ellis","sequence":"additional","affiliation":[{"name":"Department of Chemical Information, Walter Reed Army Institute of Research, Washington, DC, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jennifer","family":"Keiser","sequence":"additional","affiliation":[{"name":"Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Basel, Switzerland"},{"name":"University of Basel, Basel, Switzerland"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"235","reference":[{"issue":"3","key":"e_1_3_3_2_2","doi-asserted-by":"crossref","first-page":"403","DOI":"10.1017\/S0031182000058820","article-title":"The host-parasite relationship of Schistosoma haematobium in CBA mice","volume":"97","author":"Agnew AM","year":"1988","unstructured":"AgnewAM LucasSB DoenhoffMJ. 1988. The host-parasite relationship of Schistosoma haematobium in CBA mice. Parasitology 97(Pt. 3):403\u2013424.","journal-title":"Parasitology"},{"key":"e_1_3_3_3_2","doi-asserted-by":"crossref","first-page":"12","DOI":"10.1016\/0035-9203(92)90416-A","article-title":"Antimalarial activity in vitro of the N-desbutyl derivative of halofantrine","volume":"86","author":"Basco LK","year":"1992","unstructured":"BascoLK GillotinC GimenezF FarinottiR Le BrasJ. 1992. Antimalarial activity in vitro of the N-desbutyl derivative of halofantrine. Trans. R. Soc. Trop. Med. Hyg. 86:12\u201313.","journal-title":"Trans. R. Soc. Trop. Med. Hyg."},{"key":"e_1_3_3_4_2","doi-asserted-by":"publisher","DOI":"10.1111\/j.1365-2125.1992.tb04081.x"},{"key":"e_1_3_3_5_2","first-page":"232","article-title":"Antimalarial aminoalcohol alternatives to mefloquine","volume":"37","author":"Canfield CJ","year":"1980","unstructured":"CanfieldCJ. 1980. Antimalarial aminoalcohol alternatives to mefloquine. Acta Trop. 37:232\u2013237.","journal-title":"Acta Trop."},{"key":"e_1_3_3_6_2","doi-asserted-by":"crossref","first-page":"131","DOI":"10.1016\/0014-4894(85)90065-7","article-title":"Schistosoma haematobium: the pathology of experimental infection","volume":"59","author":"Cheever AW","year":"1985","unstructured":"CheeverAW. 1985. Schistosoma haematobium: the pathology of experimental infection. Exp. Parasitol. 59:131\u2013138.","journal-title":"Exp. Parasitol."},{"key":"e_1_3_3_7_2","doi-asserted-by":"crossref","first-page":"e477","DOI":"10.1371\/journal.pntd.0000477","article-title":"Interference with hemozoin formation represents an important mechanism of schistosomicidal action of antimalarial quinoline methanols","volume":"3","author":"Corr\u00eaa Soares JB","year":"2009","unstructured":"Corr\u00eaa SoaresJB. 2009. Interference with hemozoin formation represents an important mechanism of schistosomicidal action of antimalarial quinoline methanols. PLoS Negl. Trop. Dis. 3:e477.","journal-title":"PLoS Negl. Trop. Dis."},{"key":"e_1_3_3_8_2","doi-asserted-by":"crossref","first-page":"767","DOI":"10.4269\/ajtmh.1984.33.767","article-title":"Evaluation of the 4-pyridinemethanol WR 180,409 (enpiroline) in the treatment of induced Plasmodium falciparum infections in healthy, non-immune subjects","volume":"33","author":"Cosgriff TM","year":"1984","unstructured":"CosgriffTM. 1984. Evaluation of the 4-pyridinemethanol WR 180,409 (enpiroline) in the treatment of induced Plasmodium falciparum infections in healthy, non-immune subjects. Am. J. Trop. Med. Hyg. 33:767\u2013771.","journal-title":"Am. J. Trop. Med. Hyg."},{"key":"e_1_3_3_9_2","doi-asserted-by":"crossref","first-page":"606","DOI":"10.2307\/3281520","article-title":"Schistosoma mansoni: comparative development of schistosomules produced by artificial techniques","volume":"72","author":"Cousin CE","year":"1986","unstructured":"CousinCE StirewaltMA DorseyCH WatsonLP. 1986. Schistosoma mansoni: comparative development of schistosomules produced by artificial techniques. J. Parasitol. 72:606\u2013609.","journal-title":"J. Parasitol."},{"key":"e_1_3_3_10_2","doi-asserted-by":"crossref","first-page":"659","DOI":"10.1097\/QCO.0b013e328318978f","article-title":"Praziquantel: mechanisms of action, resistance and new derivatives for schistosomiasis","volume":"21","author":"Doenhoff MJ","year":"2008","unstructured":"DoenhoffMJ CioliD UtzingerJ. 2008. Praziquantel: mechanisms of action, resistance and new derivatives for schistosomiasis. Curr. Opin. Infect. Dis. 21:659\u2013667.","journal-title":"Curr. Opin. Infect. Dis."},{"key":"e_1_3_3_11_2","doi-asserted-by":"publisher","DOI":"10.1016\/S0006-2952(97)00510-8"},{"key":"e_1_3_3_12_2","doi-asserted-by":"crossref","first-page":"345","DOI":"10.1006\/expr.1993.1042","article-title":"Plasmodium falciparum: role of absolute stereochemistry in the antimalarial activity of synthetic amino alcohol antimalarial agents","volume":"76","author":"Karle JM","year":"1993","unstructured":"KarleJM OlmedaR GerenaL MilhousWK. 1993. Plasmodium falciparum: role of absolute stereochemistry in the antimalarial activity of synthetic amino alcohol antimalarial agents. Exp. Parasitol. 76:345\u2013351.","journal-title":"Exp. Parasitol."},{"key":"e_1_3_3_13_2","doi-asserted-by":"publisher","DOI":"10.1017\/S0031182009991739"},{"key":"e_1_3_3_14_2","doi-asserted-by":"publisher","DOI":"10.1371\/journal.pntd.0000350"},{"key":"e_1_3_3_15_2","doi-asserted-by":"crossref","first-page":"1791","DOI":"10.1093\/jac\/dkr178","article-title":"Interactions of mefloquine with praziquantel in the Schistosoma mansoni mouse model and in vitro","volume":"66","author":"Keiser J","year":"2011","unstructured":"KeiserJ ManneckT VargasM. 2011. Interactions of mefloquine with praziquantel in the Schistosoma mansoni mouse model and in vitro. J. Antimicrob. Chemother. 66:1791\u20131797.","journal-title":"J. Antimicrob. Chemother."},{"key":"e_1_3_3_16_2","doi-asserted-by":"publisher","DOI":"10.1086\/651682"},{"key":"e_1_3_3_17_2","doi-asserted-by":"crossref","first-page":"260","DOI":"10.1016\/j.exppara.2010.08.011","article-title":"Schistosoma mansoni: antischistosomal activity of the four optical isomers and the two racemates of mefloquine on schistosomula and adult worms in vitro and in vivo","volume":"127","author":"Manneck T","year":"2011","unstructured":"ManneckT BraissantO EllisW KeiserJ. 2011. Schistosoma mansoni: antischistosomal activity of the four optical isomers and the two racemates of mefloquine on schistosomula and adult worms in vitro and in vivo. Exp. Parasitol. 127:260\u2013269.","journal-title":"Exp. Parasitol."},{"key":"e_1_3_3_18_2","doi-asserted-by":"publisher","DOI":"10.1128\/JCM.02382-10"},{"key":"e_1_3_3_19_2","doi-asserted-by":"publisher","DOI":"10.1017\/S0031182009990965"},{"key":"e_1_3_3_20_2","doi-asserted-by":"crossref","first-page":"497","DOI":"10.1017\/S0031182011002204","article-title":"Mefloquine interferes with glycolysis in schistosomula of Schistosoma mansoni via inhibition of enolase","volume":"139","author":"Manneck T","year":"2012","unstructured":"ManneckT KeiserJ M\u00fcllerJ. 2012. Mefloquine interferes with glycolysis in schistosomula of Schistosoma mansoni via inhibition of enolase. Parasitology 139:497\u2013505.","journal-title":"Parasitology"},{"key":"e_1_3_3_21_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.42.11.2973"},{"key":"e_1_3_3_22_2","doi-asserted-by":"crossref","first-page":"843","DOI":"10.1086\/422759","article-title":"Inhibition of heme aggregation by chloroquine reduces Schistosoma mansoni infection","volume":"190","author":"Oliveira MF","year":"2004","unstructured":"OliveiraMF. 2004. Inhibition of heme aggregation by chloroquine reduces Schistosoma mansoni infection. J. Infect. Dis. 190:843\u2013852.","journal-title":"J. Infect. Dis."},{"key":"e_1_3_3_23_2","doi-asserted-by":"crossref","first-page":"217","DOI":"10.1016\/S0166-6851(00)00299-1","article-title":"Haemozoin in Schistosoma mansoni","volume":"111","author":"Oliveira MF","year":"2000","unstructured":"OliveiraMF. 2000. Haemozoin in Schistosoma mansoni. Mol. Biochem. Parasitol. 111:217\u2013221.","journal-title":"Mol. Biochem. Parasitol."},{"key":"e_1_3_3_24_2","doi-asserted-by":"crossref","first-page":"527","DOI":"10.1016\/j.ijpara.2003.12.003","article-title":"Sex- and stage-related sensitivity of Schistosoma mansoni to in vivo and in vitro praziquantel treatment","volume":"34","author":"Pica-Mattoccia L","year":"2004","unstructured":"Pica-MattocciaL CioliD. 2004. Sex- and stage-related sensitivity of Schistosoma mansoni to in vivo and in vitro praziquantel treatment. Int. J. Parasitol. 34:527\u2013533.","journal-title":"Int. J. Parasitol."},{"key":"e_1_3_3_25_2","doi-asserted-by":"crossref","first-page":"12","DOI":"10.1172\/JCI101949","article-title":"The use of SN-10,275 in the prophylaxis and treatment of sporozoite-induced vivax malaria, Chesson strain","volume":"27","author":"Pullman TN","year":"1948","unstructured":"PullmanTN. 1948. The use of SN-10,275 in the prophylaxis and treatment of sporozoite-induced vivax malaria, Chesson strain. J. Clin. Invest. 27:12\u201316.","journal-title":"J. Clin. Invest."},{"key":"e_1_3_3_26_2","doi-asserted-by":"publisher","DOI":"10.1517\/17460441.2.S1.S53"},{"key":"e_1_3_3_27_2","doi-asserted-by":"crossref","first-page":"1593","DOI":"10.1017\/S0031182009990552","article-title":"A wake up call for urinary schistosomiasis: reconciling research effort with public health importance","volume":"136","author":"Rollinson D","year":"2009","unstructured":"RollinsonD. 2009. A wake up call for urinary schistosomiasis: reconciling research effort with public health importance. Parasitology 136:1593\u20131610.","journal-title":"Parasitology"},{"key":"e_1_3_3_28_2","doi-asserted-by":"crossref","first-page":"366","DOI":"10.1021\/jm00308a041","article-title":"Laboratory evaluation of the phototoxic potency of quinolinemethanols","volume":"11","author":"Rothe WE","year":"1968","unstructured":"RotheWE JacobusDP. 1968. Laboratory evaluation of the phototoxic potency of quinolinemethanols. J. Med. Chem. 11:366\u2013368.","journal-title":"J. Med. Chem."},{"key":"e_1_3_3_29_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.14.3.420"},{"key":"e_1_3_3_30_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.13.6.1011"},{"key":"e_1_3_3_31_2","doi-asserted-by":"publisher","DOI":"10.1016\/S1473-3099(06)70521-7"},{"key":"e_1_3_3_32_2","doi-asserted-by":"crossref","first-page":"68","DOI":"10.1111\/j.1476-5381.1959.tb00930.x","article-title":"Studies of a proteolytic enzyme from Schistosoma mansoni","volume":"14","author":"Timms AR","year":"1959","unstructured":"TimmsAR BuedingE. 1959. Studies of a proteolytic enzyme from Schistosoma mansoni. Br. J. Pharmacol. Chemother. 14:68\u201373.","journal-title":"Br. J. Pharmacol. Chemother."},{"key":"e_1_3_3_33_2","doi-asserted-by":"crossref","first-page":"263","DOI":"10.1517\/14656566.5.2.263","article-title":"Schistosomiasis and soil-transmitted helminthiasis: common drugs for treatment and control","volume":"5","author":"Utzinger J","year":"2004","unstructured":"UtzingerJ KeiserJ. 2004. Schistosomiasis and soil-transmitted helminthiasis: common drugs for treatment and control. Expert Opin. Pharmacother. 5:263\u2013285.","journal-title":"Expert Opin. Pharmacother."},{"key":"e_1_3_3_34_2","doi-asserted-by":"crossref","first-page":"253","DOI":"10.1016\/j.tmaid.2008.06.006","article-title":"Schistosomicidal activity of the antimalarial drug, mefloquine, in Schistosoma mansoni-infected mice","volume":"6","author":"Van Nassauw L","year":"2008","unstructured":"Van NassauwL TooveyS Van Op den BoschJ TimmermansJP VercruysseJ. 2008. Schistosomicidal activity of the antimalarial drug, mefloquine, in Schistosoma mansoni-infected mice. Travel Med. Infect. Dis. 6:253\u2013258.","journal-title":"Travel Med. Infect. Dis."},{"key":"e_1_3_3_35_2","first-page":"73","article-title":"Schistosomiasis: number of people treated in 2009","volume":"86","author":"World Health Organization","year":"2011","unstructured":"World Health Organization. 2011. Schistosomiasis: number of people treated in 2009. Wkly. Epidemiol. Rec. 86:73\u201380.","journal-title":"Wkly. Epidemiol. Rec."},{"key":"e_1_3_3_36_2","volume-title":"Preventive chemotherapy in human helminthiasis","author":"World Health Organization","year":"2006","unstructured":"World Health Organization. 2006. Preventive chemotherapy in human helminthiasis. World Health Organization, Geneva, Switzerland."},{"key":"e_1_3_3_37_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.01537-06"},{"key":"e_1_3_3_38_2","doi-asserted-by":"crossref","first-page":"399","DOI":"10.1007\/s00436-010-2080-y","article-title":"Effect of mefloquine administered orally at single, multiple, or combined with artemether, artesunate, or praziquantel in treatment of mice infected with Schistosoma japonicum","volume":"108","author":"Xiao SH","year":"2011","unstructured":"XiaoSH MeiJY JiaoPY. 2011. Effect of mefloquine administered orally at single, multiple, or combined with artemether, artesunate, or praziquantel in treatment of mice infected with Schistosoma japonicum. Parasitol. Res. 108:399\u2013406.","journal-title":"Parasitol. Res."}],"container-title":["Antimicrobial Agents and Chemotherapy"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/journals.asm.org\/doi\/pdf\/10.1128\/AAC.06177-11","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/journals.asm.org\/doi\/pdf\/10.1128\/AAC.06177-11","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2022,2,21]],"date-time":"2022-02-21T22:20:08Z","timestamp":1645482008000},"score":1,"resource":{"primary":{"URL":"https:\/\/journals.asm.org\/doi\/10.1128\/AAC.06177-11"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2012,6]]},"references-count":37,"journal-issue":{"issue":"6","published-print":{"date-parts":[[2012,6]]}},"alternative-id":["10.1128\/AAC.06177-11"],"URL":"https:\/\/doi.org\/10.1128\/aac.06177-11","relation":{},"ISSN":["0066-4804","1098-6596"],"issn-type":[{"value":"0066-4804","type":"print"},{"value":"1098-6596","type":"electronic"}],"subject":[],"published":{"date-parts":[[2012,6]]},"assertion":[{"value":"2011-11-26","order":0,"name":"received","label":"Received","group":{"name":"publication_history","label":"Publication History"}},{"value":"2012-03-23","order":1,"name":"accepted","label":"Accepted","group":{"name":"publication_history","label":"Publication History"}},{"value":"2012-05-13","order":2,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}]}}