{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,3,31]],"date-time":"2026-03-31T17:02:41Z","timestamp":1774976561831,"version":"3.50.1"},"reference-count":20,"publisher":"American Society for Microbiology","issue":"5","license":[{"start":{"date-parts":[[2017,5,1]],"date-time":"2017-05-01T00:00:00Z","timestamp":1493596800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.asm.org\/non-commercial-tdm-license"}],"funder":[{"name":"Global Alliance for Livestock Veterinary Medicines","award":["STP-R55A0532"],"award-info":[{"award-number":["STP-R55A0532"]}]}],"content-domain":{"domain":["journals.asm.org"],"crossmark-restriction":true},"short-container-title":["Antimicrob Agents Chemother"],"published-print":{"date-parts":[[2017,5]]},"abstract":"<jats:title>ABSTRACT<\/jats:title>\n          <jats:p>\n            African animal trypanosomosis (AAT) is caused by the tsetse fly-transmitted protozoans\n            <jats:named-content content-type=\"genus-species\">Trypanosoma congolense<\/jats:named-content>\n            and\n            <jats:named-content content-type=\"genus-species\">T. vivax<\/jats:named-content>\n            and leads to huge agricultural losses throughout sub-Saharan Africa. Three drugs are available to treat nagana in cattle (diminazene diaceturate, homidium chloride, and isometamidium chloride). With increasing reports of drug-resistant populations, new molecules should be investigated as potential candidates to combat nagana. Dicationic compounds have been demonstrated to have excellent efficacy against different kinetoplastid parasites. This study therefore evaluated the activities of 37 diamidines, using\n            <jats:italic>in vitro<\/jats:italic>\n            and\n            <jats:italic>ex vivo<\/jats:italic>\n            drug sensitivity assays. The 50% inhibitory concentrations obtained ranged from 0.007 to 0.562 \u03bcg\/ml for\n            <jats:named-content content-type=\"genus-species\">T. congolense<\/jats:named-content>\n            and from 0.019 to 0.607 \u03bcg\/ml for\n            <jats:named-content content-type=\"genus-species\">T. vivax<\/jats:named-content>\n            . On the basis of these promising results, 33 of these diamidines were further examined using\n            <jats:italic>in vivo<\/jats:italic>\n            mouse models of infection. Minimal curative doses of 1.25 mg\/kg of body weight for both\n            <jats:named-content content-type=\"genus-species\">T. congolense<\/jats:named-content>\n            - and\n            <jats:named-content content-type=\"genus-species\">T. vivax<\/jats:named-content>\n            -infected mice were seen when the diamidines were administered intraperitoneally (i.p.) over 4 consecutive days. From these observations, 15 of these 33 diamidines were then further tested\n            <jats:italic>in vivo<\/jats:italic>\n            , using a single bolus dose for administration. The total cure of mice infected with\n            <jats:named-content content-type=\"genus-species\">T. congolense<\/jats:named-content>\n            and\n            <jats:named-content content-type=\"genus-species\">T. vivax<\/jats:named-content>\n            was seen with single i.p. doses of 5 and 2.5 mg\/kg, respectively. This study identified a selection of diamidines which could be considered lead compounds for the treatment of nagana.\n          <\/jats:p>","DOI":"10.1128\/aac.02356-16","type":"journal-article","created":{"date-parts":[[2017,2,14]],"date-time":"2017-02-14T01:55:24Z","timestamp":1487037324000},"update-policy":"https:\/\/doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":11,"title":["<i>In Vitro<\/i>\n            ,\n            <i>Ex Vivo<\/i>\n            , and\n            <i>In Vivo<\/i>\n            Activities of Diamidines against Trypanosoma congolense and Trypanosoma vivax"],"prefix":"10.1128","volume":"61","author":[{"given":"Kirsten","family":"Gillingwater","sequence":"first","affiliation":[{"name":"Parasite Chemotherapy, Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Basel, Switzerland"},{"name":"University of Basel, Basel, Switzerland"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Christina","family":"Kunz","sequence":"additional","affiliation":[{"name":"Parasite Chemotherapy, Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Basel, Switzerland"},{"name":"University of Basel, Basel, Switzerland"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Christiane","family":"Braghiroli","sequence":"additional","affiliation":[{"name":"Parasite Chemotherapy, Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Basel, Switzerland"},{"name":"University of Basel, Basel, Switzerland"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"David W.","family":"Boykin","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Georgia State University, Atlanta, Georgia, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Richard R.","family":"Tidwell","sequence":"additional","affiliation":[{"name":"Department of Pathology, University of North Carolina, Chapel Hill, North Carolina, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Reto","family":"Brun","sequence":"additional","affiliation":[{"name":"Parasite Chemotherapy, Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Basel, Switzerland"},{"name":"University of Basel, Basel, Switzerland"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"235","reference":[{"key":"e_1_3_2_2_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.prevetmed.2013.10.024"},{"key":"e_1_3_2_3_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.actatropica.2008.02.003"},{"key":"e_1_3_2_4_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.drup.2008.10.002"},{"key":"e_1_3_2_5_2","doi-asserted-by":"publisher","DOI":"10.1371\/journal.pntd.0001454"},{"key":"e_1_3_2_6_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.vetpar.2011.12.019"},{"key":"e_1_3_2_7_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.vetpar.2012.04.022"},{"key":"e_1_3_2_8_2","doi-asserted-by":"publisher","DOI":"10.1186\/1756-3305-5-155"},{"key":"e_1_3_2_9_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.00225-09"},{"key":"e_1_3_2_10_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.01482-10"},{"key":"e_1_3_2_11_2","doi-asserted-by":"publisher","DOI":"10.1371\/journal.pntd.0001734"},{"key":"e_1_3_2_12_2","first-page":"147","article-title":"Diamidines as antitrypanosomal, antileishmanial and antimalarial agents","volume":"7","author":"Werbovetz K","year":"2006","unstructured":"Werbovetz K . 2006. Diamidines as antitrypanosomal, antileishmanial and antimalarial agents. Curr Opin Investig Drugs7:147\u2013157.","journal-title":"Curr Opin Investig Drugs"},{"key":"e_1_3_2_13_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.00422-09"},{"key":"e_1_3_2_14_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.vetpar.2010.01.019"},{"key":"e_1_3_2_15_2","doi-asserted-by":"publisher","DOI":"10.1371\/journal.pone.0020836"},{"key":"e_1_3_2_16_2","doi-asserted-by":"publisher","DOI":"10.1016\/0001-706X(89)90048-X"},{"key":"e_1_3_2_17_2","doi-asserted-by":"publisher","DOI":"10.1016\/0014-4894(74)90107-6"},{"key":"e_1_3_2_18_2","first-page":"211","article-title":"Sleeping sickness survey in Musoma District, Tanzania. IV. Examination of wild mammals as a potential reservoir for T rhodesiense","volume":"28","author":"Geigy R","year":"1971","unstructured":"Geigy R MwambuPMKauffmannM. 1971. Sleeping sickness survey in Musoma District, Tanzania. IV. Examination of wild mammals as a potential reservoir for T rhodesiense. Acta Trop28:211\u2013220.","journal-title":"Acta Trop"},{"key":"e_1_3_2_19_2","doi-asserted-by":"publisher","DOI":"10.1186\/1756-3305-5-71"},{"key":"e_1_3_2_20_2","first-page":"135","article-title":"In vitro cultivation of animal-infective forms of a West African Trypanosoma vivax stock","volume":"39","author":"Brun R","year":"1982","unstructured":"Brun R MolooSK. 1982. In vitro cultivation of animal-infective forms of a West African Trypanosoma vivax stock. Acta Trop39:135\u2013141.","journal-title":"Acta Trop"},{"key":"e_1_3_2_21_2","doi-asserted-by":"publisher","DOI":"10.1016\/S0001-706X(97)00079-X"}],"container-title":["Antimicrobial Agents and Chemotherapy"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/journals.asm.org\/doi\/pdf\/10.1128\/AAC.02356-16","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/journals.asm.org\/doi\/pdf\/10.1128\/AAC.02356-16","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2022,2,21]],"date-time":"2022-02-21T20:53:24Z","timestamp":1645476804000},"score":1,"resource":{"primary":{"URL":"https:\/\/journals.asm.org\/doi\/10.1128\/AAC.02356-16"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2017,5]]},"references-count":20,"journal-issue":{"issue":"5","published-print":{"date-parts":[[2017,5]]}},"alternative-id":["10.1128\/AAC.02356-16"],"URL":"https:\/\/doi.org\/10.1128\/aac.02356-16","relation":{},"ISSN":["0066-4804","1098-6596"],"issn-type":[{"value":"0066-4804","type":"print"},{"value":"1098-6596","type":"electronic"}],"subject":[],"published":{"date-parts":[[2017,5]]},"assertion":[{"value":"2016-11-06","order":0,"name":"received","label":"Received","group":{"name":"publication_history","label":"Publication History"}},{"value":"2017-01-22","order":1,"name":"accepted","label":"Accepted","group":{"name":"publication_history","label":"Publication History"}},{"value":"2017-04-24","order":2,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}],"article-number":"e02356-16"}}