{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,12]],"date-time":"2025-10-12T20:22:29Z","timestamp":1760300549935,"version":"3.37.3"},"reference-count":45,"publisher":"Georg Thieme Verlag KG","issue":"06","funder":[{"name":"South African Medical Research Council (MRC) with funds from National Treasury under its Economic Competitiveness and Support Package awarded to Prof. Heinrich Hoppe, Rhodes University"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Drug Res (Stuttg)"],"published-print":{"date-parts":[[2021,7]]},"abstract":"<jats:p>Sleeping sickness, caused by trypanosomes, is a debilitating,\n                  neglected tropical disease wherein current treatments suffer\n                  from several drawbacks such as toxicity, low activity, and\n                  poor pharmacokinetic properties, and hence the need for\n                  alternative treatment is apparent. To this effect, we\n                  screened in vitro a library of 2-quinazolinone derivatives\n                  for antitrypanosomal activity against T.b. brucei and\n                  cytotoxicity against HeLa cells. Seven compounds having no\n                  overt cytotoxicity against HeLa cells exhibited\n                  antitrypanosomal activity in the range of 0.093\u201345\u2009\u00b5M were\n                  identified. The activity data suggests that the\n                  antitrypanosomal activity of this compound class is amenable\n                  to substituents at N1 and C6 positions. Compound 14\n                  having a molecular weight of 238Da, ClogP value of 1 and a\n                  total polar surface area of 49 was identified as the most\n                  active, exhibiting an IC50 value of 0.093\u2009\u00b5M\n                  Graphical\n                          Abstract.\n          <\/jats:p>","DOI":"10.1055\/a-1349-1256","type":"journal-article","created":{"date-parts":[[2021,2,4]],"date-time":"2021-02-04T00:43:44Z","timestamp":1612399424000},"page":"335-340","source":"Crossref","is-referenced-by-count":1,"title":["In-vitro Anti-trypanosomal and Cytotoxicity Evaluation of\n                                        3-methyl-3,4-dihydroquinazolin-2(1H)-one Derivatives"],"prefix":"10.1055","volume":"71","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-6152-9467","authenticated-orcid":false,"given":"Omobolanle J.","family":"Jesumoroti","sequence":"additional","affiliation":[{"name":"Centre of Excellence for Pharmaceutical Sciences,\n                                        North-West University, Potchefstroom, South\n                                        Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Richard M.","family":"Beteck","sequence":"additional","affiliation":[{"name":"Centre of Excellence for Pharmaceutical Sciences,\n                                        North-West University, Potchefstroom, South\n                                        Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Lesetja J.","family":"Legoabe","sequence":"additional","affiliation":[{"name":"Centre of Excellence for Pharmaceutical Sciences,\n                                        North-West University, Potchefstroom, South\n                                        Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"194","published-online":{"date-parts":[[2021,2,3]]},"reference":[{"key":"ref1","doi-asserted-by":"crossref","first-page":"906","DOI":"10.1046\/j.1365-3156.2001.00775.x","article-title":"The phenomenon of treatment failures in human African\n                                        trypanosomiasis","volume":"6","author":"R Brun","year":"2001","journal-title":"Trop Med Int Health"},{"key":"ref2","doi-asserted-by":"crossref","first-page":"1469","DOI":"10.1016\/S0140-6736(03)14694-6","article-title":"The trypanosomiases","volume":"362","author":"M Barrett","year":"2003","journal-title":"Lancet"},{"key":"ref3","doi-asserted-by":"crossref","first-page":"337","DOI":"10.1055\/a-0775-0737","article-title":"In vitro anti-trypanosomal activities of indanone-based\n                                        chalcones","volume":"69","author":"R Beteck","year":"2019","journal-title":"Drug 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treatment\n                                        of human African trypanosomiasis","volume":"107","author":"P Babokhov","year":"2013","journal-title":"Pathogens and Global Health"},{"key":"ref24","doi-asserted-by":"crossref","first-page":"610","DOI":"10.1002\/ardp.201300158","article-title":"Synthesis and Biological evaluation of a novel series of 6, 8-D\n                                        ibromo-4 (3 H) quinazolinone derivatives as anticancer\n                                        agents","volume":"346","author":"M Ahmed","year":"2013","journal-title":"Archiv der Pharmazie"},{"key":"ref25","doi-asserted-by":"crossref","first-page":"217","DOI":"10.1038\/nrmicro.2016.193","article-title":"Antitrypanosomatid drug discovery: An ongoing challenge and a\n                                        continuing need","volume":"15","author":"M Field","year":"2017","journal-title":"Nat Rev 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               the coping strategies of households in the South Western\n                                        Kenya foci","volume":"11","author":"S Bukachi","year":"2017","journal-title":"PLoS Negl Trop Dis"},{"key":"ref39","doi-asserted-by":"crossref","first-page":"391","DOI":"10.1007\/s11030-019-09960-5","article-title":"The monoamine oxidase inhibition properties of C6-and\n                                        N1-substituted\n                                        3-methyl-3,4-dihydroquinazolin-2(1H)-one\n                                        derivatives","volume":"24","author":"L Marais","year":"2019","journal-title":"Molecular Diversity"},{"key":"ref40","doi-asserted-by":"crossref","first-page":"5522","DOI":"10.1021\/acs.jmedchem.5b00515","article-title":"Protozoan parasite growth inhibitors discovered by\n                                        cross-screening yield potent scaffolds for lead\n                                        discovery","volume":"58","author":"W Devine","year":"2015","journal-title":"J Med Chem"},{"key":"ref41","doi-asserted-by":"crossref","first-page":"1751","DOI":"10.1002\/cmdc.201800404","article-title":"Brain-penetrant, triazolopyrimidine and phenylpyrimidine\n                                        microtubule-stabilizers as potential leads to treat Human\n                                        African Trypanosomiasis","volume":"13","author":"L Monti","year":"2018","journal-title":"ChemMedChem"},{"key":"ref42","doi-asserted-by":"crossref","first-page":"206","DOI":"10.3390\/medicina55050206","article-title":"Anti-Trypanosomal and antimalarial properties of tetralone\n                                        derivatives and structurally related\n                                        benzocycloalkanones","volume":"55","author":"R Beteck","year":"2019","journal-title":"Medicina (Kaunas)"},{"key":"ref43","doi-asserted-by":"crossref","first-page":"660","DOI":"10.1007\/BF03402046","article-title":"Chalcone, acyl hydrazide, and related amides kill cultured\n                                        Trypanosoma brucei brucei","volume":"6","author":"L Troeberg","year":"2000","journal-title":"Mol Med"},{"key":"ref44","doi-asserted-by":"crossref","first-page":"2037","DOI":"10.1039\/C8MD00319J","article-title":"Screening of the Pathogen Box reveals new starting points for\n                                        anti-trypanosomal drug discovery","volume":"9","author":"C Veale","year":"2018","journal-title":"Med Chem Commun"},{"key":"ref45","doi-asserted-by":"crossref","first-page":"217","DOI":"10.1038\/nrmicro.2016.193","article-title":"Antitrypanosomatid drug discovery: an ongoing challenge and a\n                                        continuing need","volume":"15","author":"M Field","year":"2017","journal-title":"Nat Rev Microbiol"},{"key":"ref46","doi-asserted-by":"publisher","first-page":"188","DOI":"10.17159\/0379-4350\/2018","article-title":"Synthesis, in vitro cytotoxicity and trypanocidal evaluation of\n                                        novel 1,3,6-substituted non-fluoroquinolones","volume":"71","author":"R Beteck","year":"2018","journal-title":"S Afr J Chem"},{"key":"ref47","doi-asserted-by":"crossref","first-page":"265","DOI":"10.2174\/1573406414666181005145042","article-title":"Synthesis, 2D-QSAR studies and biological evaluation of\n                                        quinazoline derivatives as potent anti-trypanosoma cruzi\n                                        agents","volume":"15","author":"M Bollini","year":"2019","journal-title":"J Medicinal Chemistry"}],"container-title":["Drug 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