{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,18]],"date-time":"2026-08-18T01:30:11Z","timestamp":1787016611451,"version":"build-2736575974"},"reference-count":48,"publisher":"American Society for Microbiology","issue":"7","license":[{"start":{"date-parts":[[2016,7,1]],"date-time":"2016-07-01T00:00:00Z","timestamp":1467331200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.asm.org\/non-commercial-tdm-license"}],"funder":[{"DOI":"10.13039\/501100001412","name":"Council of Scientific and Industrial Research","doi-asserted-by":"publisher","award":["SPlenDID BSC 0104"],"award-info":[{"award-number":["SPlenDID BSC 0104"]}],"id":[{"id":"10.13039\/501100001412","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":[[2016,7]]},"abstract":"<jats:title>ABSTRACT<\/jats:title>\n                  <jats:p>\n                    We synthesized a new series of conjugated hydrazones that were found to be active against malaria parasite\n                    <jats:italic>in vitro<\/jats:italic>\n                    , as well as\n                    <jats:italic>in vivo<\/jats:italic>\n                    in a murine model. These hydrazones concentration-dependently chelated free iron and offered antimalarial activity. Upon screening of the synthesized hydrazones, compound 5f was found to be the most active iron chelator, as well as antiplasmodial. Compound 5f also interacted with free heme (\n                    <jats:italic>\n                      K\n                      <jats:sub>D<\/jats:sub>\n                    <\/jats:italic>\n                    [equilibrium dissociation constant] = 1.17 \u00b1 0.8 \u03bcM), an iron-containing tetrapyrrole released after hemoglobin digestion by the parasite, and inhibited heme polymerization by parasite lysate. Structure-activity relationship studies indicated that a nitrogen- and sulfur-substituted five-membered aromatic ring present within the benzothiazole hydrazones might be responsible for their antimalarial activity. The dose-dependent antimalarial and heme polymerization inhibitory activities of the lead compound 5f were further validated by following [\n                    <jats:sup>3<\/jats:sup>\n                    H]hypoxanthine incorporation and hemozoin formation in parasite, respectively. It is worth mentioning that compound 5f exhibited antiplasmodial activity\n                    <jats:italic>in vitro<\/jats:italic>\n                    against a chloroquine\/pyrimethamine-resistant strain of\n                    <jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">Plasmodium falciparum<\/jats:named-content>\n                    (K1). We also evaluated\n                    <jats:italic>in vivo<\/jats:italic>\n                    antimalarial activity of compound 5f in a murine model where a lethal multiple-drug-resistant strain of\n                    <jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">Plasmodium yoelii<\/jats:named-content>\n                    was used to infect Swiss albino mice. Compound 5f significantly suppressed the growth of parasite, and the infected mice experienced longer life spans upon treatment with this compound. During\n                    <jats:italic>in vitro<\/jats:italic>\n                    and\n                    <jats:italic>in vivo<\/jats:italic>\n                    toxicity assays, compound 5f showed minimal alteration in biochemical and hematological parameters compared to control. In conclusion, we identified a new class of hydrazone with therapeutic potential against malaria.\n                  <\/jats:p>","DOI":"10.1128\/aac.01575-15","type":"journal-article","created":{"date-parts":[[2016,5,2]],"date-time":"2016-05-02T22:19:05Z","timestamp":1462227545000},"page":"4217-4228","update-policy":"https:\/\/doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":76,"title":["Antimalarial Activity of Small-Molecule Benzothiazole Hydrazones"],"prefix":"10.1128","volume":"60","author":[{"given":"Souvik","family":"Sarkar","sequence":"first","affiliation":[{"name":"Division of Infectious Diseases and Immunology, CSIR-Indian Institute of Chemical Biology, Jadavpur, Kolkata, West Bengal, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Asim A.","family":"Siddiqui","sequence":"additional","affiliation":[{"name":"Division of Infectious Diseases and Immunology, CSIR-Indian Institute of Chemical Biology, Jadavpur, Kolkata, West Bengal, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shubhra J.","family":"Saha","sequence":"additional","affiliation":[{"name":"Division of Infectious Diseases and Immunology, CSIR-Indian Institute of Chemical Biology, Jadavpur, Kolkata, West Bengal, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Rudranil","family":"De","sequence":"additional","affiliation":[{"name":"Division of Infectious Diseases and Immunology, CSIR-Indian Institute of Chemical Biology, Jadavpur, Kolkata, West Bengal, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Somnath","family":"Mazumder","sequence":"additional","affiliation":[{"name":"Division of Infectious Diseases and Immunology, CSIR-Indian Institute of Chemical Biology, Jadavpur, Kolkata, West Bengal, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chinmoy","family":"Banerjee","sequence":"additional","affiliation":[{"name":"Division of Infectious Diseases and Immunology, CSIR-Indian Institute of Chemical Biology, Jadavpur, Kolkata, West Bengal, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mohd S.","family":"Iqbal","sequence":"additional","affiliation":[{"name":"Division of Infectious Diseases and Immunology, CSIR-Indian Institute of Chemical Biology, Jadavpur, Kolkata, West Bengal, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shiladitya","family":"Nag","sequence":"additional","affiliation":[{"name":"Division of Infectious Diseases and Immunology, CSIR-Indian Institute of Chemical Biology, Jadavpur, Kolkata, West Bengal, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Susanta","family":"Adhikari","sequence":"additional","affiliation":[{"name":"Department of Chemistry, University of Calcutta, Kolkata, West Bengal, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Uday","family":"Bandyopadhyay","sequence":"additional","affiliation":[{"name":"Division of Infectious Diseases and Immunology, CSIR-Indian Institute of Chemical Biology, Jadavpur, Kolkata, West Bengal, India"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"235","reference":[{"key":"e_1_3_2_2_2","doi-asserted-by":"publisher","DOI":"10.1006\/scel.1993.1042"},{"key":"e_1_3_2_3_2","doi-asserted-by":"publisher","DOI":"10.1098\/rstb.2011.0091"},{"key":"e_1_3_2_4_2","doi-asserted-by":"publisher","DOI":"10.1586\/ecp.09.28"},{"key":"e_1_3_2_5_2","doi-asserted-by":"publisher","DOI":"10.1172\/JCI21682"},{"key":"e_1_3_2_6_2","doi-asserted-by":"publisher","DOI":"10.1016\/S0166-6851(02)00282-7"},{"key":"e_1_3_2_7_2","doi-asserted-by":"publisher","DOI":"10.1080\/03602530903178905"},{"key":"e_1_3_2_8_2","doi-asserted-by":"publisher","DOI":"10.1017\/S0031182009991880"},{"key":"e_1_3_2_9_2","doi-asserted-by":"crossref","first-page":"593","DOI":"10.4269\/ajtmh.1991.45.593","article-title":"Stage-specific ultrastructural effects of desferrioxamine on Plasmodium falciparum in vitro","volume":"45","author":"Atkinson CT","year":"1991","unstructured":"Atkinson CT, Bayne MT, Gordeuk VR, Brittenham GM, Aikawa M. 1991. 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