{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,3,29]],"date-time":"2026-03-29T13:54:39Z","timestamp":1774792479092,"version":"3.50.1"},"reference-count":25,"publisher":"Bentham Science Publishers Ltd.","issue":"4","content-domain":{"domain":["eurekaselect.com"],"crossmark-restriction":true},"short-container-title":["MC"],"published-print":{"date-parts":[[2019,5,20]]},"abstract":"<jats:sec>\n<jats:title>Background:<\/jats:title>\n<jats:p>Human African Trypanosomiasis (HAT, sleeping sickness) and Malaria\nboth are insect vectored tropical diseases. Only a couple of drugs is able to cure HAT, but all of\nthem are toxic, prone to resistance and require parenteral administration. Malaria is responsible for\nhigh morbidity and mortality in humans. It is one of the global killers of children. Wide-spread\ndrug resistance against traditional therapeutics which were once highly effective makes them almost\nuseless. Therefore new drugs against both diseases are urgently needed.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Objective:<\/jats:title>\n<jats:p>Recently, we reported the synthesis and antiprotozoal activities of a number of new 2-\nsubstituted 4-carbamoyl- and 4-aminoquinolines. This study focussed on the synthesis of novel\ntetrazole derivatives which are linked to the quinoline core via a piperidine ring.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Methods:<\/jats:title>\n<jats:p>Novel compounds exhibiting a 7-chloroquinoline and a tetrazole ring were prepared via\nUgi-azide reaction. Modifications were restricted to the orientation and the substitution of the\nlinker. Compounds were tested for their activities against Trypanosoma brucei rhodesiense (STIB\n900). Their antiplasmodial activities were determined against a sensitive (NF54) and a multiresistant\nstrain (K1) of Plasmodium falciparum.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Results:<\/jats:title>\n<jats:p>Eighteen tetrazole derivatives were prepared. The results of the biological tests were compared\nwith the activities of drugs in use and structure-activity relationships were discussed. Their\nantitrypanosomal activities were only moderate. In contrast some of the compounds showed\npromising activity against both strains of Plasmodium falciparum and good to excellent resistance\nindices.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Conclusion:<\/jats:title>\n<jats:p>The antiplasmodial activities depended on the orientation of the 4-aminopiperidine\nlinker. Compounds with a tertiary amino group in position 4 of the quinoline ring exhibited equal\nactivity against both strains, whereas those with a secondary amino group were mainly active\nagainst the sensitive strain.<\/jats:p>\n<\/jats:sec>","DOI":"10.2174\/1573406414666181015115101","type":"journal-article","created":{"date-parts":[[2018,10,16]],"date-time":"2018-10-16T08:08:13Z","timestamp":1539677293000},"page":"409-416","update-policy":"https:\/\/doi.org\/10.2174\/bsp_crossmark_policy","source":"Crossref","is-referenced-by-count":13,"title":["Antiprotozoal Activities of Tetrazole-quinolines with Aminopiperidine Linker"],"prefix":"10.2174","volume":"15","author":[{"given":"Patrick","family":"Hochegger","sequence":"first","affiliation":[{"name":"Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, University of Graz, Graz, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Johanna","family":"Faist","sequence":"additional","affiliation":[{"name":"Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, University of Graz, Graz, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Werner","family":"Seebacher","sequence":"additional","affiliation":[{"name":"Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, University of Graz, Graz, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Robert","family":"Saf","sequence":"additional","affiliation":[{"name":"Institute for Chemistry and Technology of Materials (ICTM), University of Technology, Graz, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Pascal","family":"M\u00e4ser","sequence":"additional","affiliation":[{"name":"Swiss Tropical and Public Health Institute and University of Basel, Basel, Switzerland"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Marcel","family":"Kaiser","sequence":"additional","affiliation":[{"name":"Swiss Tropical and Public Health Institute and University of Basel, Basel, Switzerland"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Robert","family":"Weis","sequence":"additional","affiliation":[{"name":"Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, University of Graz, Graz, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"965","reference":[{"key":"ref=1","unstructured":"World Health Organization 2017, Human African trypanosomiasis;\nAvailable from: http:\/\/www.who.int\/trypanosomiasis_african\/\nnews\/HAT_elimination_on_track\/en\/"},{"key":"ref=2","unstructured":"World Health Organization, Human African Trypanosomiasis, Fact\nsheet N\u00b0259, updated January 2017."},{"key":"ref=3","unstructured":"World Health Organization, Human African trypanosomiasis;\nSymptoms, diagnosis & treatment. 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