{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,17]],"date-time":"2026-10-17T19:12:57Z","timestamp":1792264377354,"version":"4.4.0"},"reference-count":39,"publisher":"American Society for Microbiology","issue":"9","license":[{"start":{"date-parts":[[2016,9,1]],"date-time":"2016-09-01T00:00:00Z","timestamp":1472688000000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.asm.org\/non-commercial-tdm-license"}],"funder":[{"DOI":"10.13039\/100000057","name":"HHS | NIH | National Institute of General Medical Sciences","doi-asserted-by":"publisher","award":["8P20GM103447"],"award-info":[{"award-number":["8P20GM103447"]}],"id":[{"id":"10.13039\/100000057","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100000781","name":"EC | European Research Council","doi-asserted-by":"publisher","award":["ERC-2013-CoG 614739-A_HERO"],"award-info":[{"award-number":["ERC-2013-CoG 614739-A_HERO"]}],"id":[{"id":"10.13039\/501100000781","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100001309","name":"Research Corporation for Science Advancement","doi-asserted-by":"publisher","award":["HR13-157"],"award-info":[{"award-number":["HR13-157"]}],"id":[{"id":"10.13039\/100001309","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["journals.asm.org"],"crossmark-restriction":true},"short-container-title":["Antimicrob Agents Chemother"],"published-print":{"date-parts":[[2016,9]]},"abstract":"<jats:title>ABSTRACT<\/jats:title>\n          <jats:p>\n            Praziquantel (PZQ) is the only drug available for the treatment of schistosomiasis, and since its large-scale use might be associated with the onset of resistance, new antischistosomal drugs should be developed. A series of 26 synthetic tetraazamacrocyclic derivatives and their metal complexes were synthesized, characterized, and screened for antischistosomal activity by application of a phased screening program. The compounds were first screened against newly transformed schistosomula (NTS) of harvested\n            <jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">Schistosoma mansoni<\/jats:named-content>\n            cercariae, then against adult worms, and finally,\n            <jats:italic>in vivo<\/jats:italic>\n            using the mouse model of\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            infection. At a concentration of 33 \u03bcM, incubation with a total of 12 compounds resulted in the mortality of NTS at the 62% to 100% level. Five of these showing 100% inhibition of viability of NTS at 10 \u03bcM were selected for further screening for determination of the 50 inhibitory concentrations (IC\n            <jats:sub>50<\/jats:sub>\n            s) against both NTS and adult worms. Against NTS, all 5 compounds showed IC\n            <jats:sub>50<\/jats:sub>\n            s comparable to the IC\n            <jats:sub>50<\/jats:sub>\n            of the standard drug, PZQ (0.87 to 9.65 \u03bcM for the 5 compounds versus 2.20 \u03bcM for PZQ). Three of these, which are the bisquinoline derivative of cyclen and its Fe\n            <jats:sup>2+<\/jats:sup>\n            and Mn\n            <jats:sup>2+<\/jats:sup>\n            complexes, showed micromolar IC\n            <jats:sub>50<\/jats:sub>\n            s (1.62 \u03bcM, 1.34 \u03bcM, and 4.12 \u03bcM, respectively, versus 0.10 \u03bcM for PZQ) against adult worms.\n            <jats:italic>In vivo<\/jats:italic>\n            , the worm burden reductions were 12.3%, 88.4%, and 74.5%, respectively, at a single oral dose of 400 mg\/kg of body weight. The Fe\n            <jats:sup>2+<\/jats:sup>\n            complex exhibited activity\n            <jats:italic>in vivo<\/jats:italic>\n            comparable to that of PZQ, pointing to the discovery of a novel drug lead for schistosomiasis.\n          <\/jats:p>","DOI":"10.1128\/aac.00778-16","type":"journal-article","created":{"date-parts":[[2016,6,22]],"date-time":"2016-06-22T03:08:33Z","timestamp":1466564913000},"page":"5331-5336","update-policy":"https:\/\/doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":30,"title":["Discovery of Antischistosomal Drug Leads Based on Tetraazamacrocyclic Derivatives and Their Metal Complexes"],"prefix":"10.1128","volume":"60","author":[{"given":"M. O. Faruk","family":"Khan","sequence":"first","affiliation":[{"name":"College of Pharmacy, Southwestern Oklahoma State University, Weatherford, Oklahoma, 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"}]},{"given":"P. N. A.","family":"Amoyaw","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Southwestern Oklahoma State University, Weatherford, Oklahoma, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mohammad F.","family":"Hossain","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Southwestern Oklahoma State University, Weatherford, Oklahoma, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mireille","family":"Vargas","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"}]},{"given":"Justin G.","family":"Le","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Southwestern Oklahoma State University, Weatherford, Oklahoma, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Natalie C.","family":"Simpson","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Southwestern Oklahoma State University, Weatherford, Oklahoma, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kimberly D.","family":"Roewe","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Southwestern Oklahoma State University, Weatherford, Oklahoma, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"TaRynn N. 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