{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,12,4]],"date-time":"2025-12-04T19:20:51Z","timestamp":1764876051092,"version":"3.46.0"},"reference-count":33,"publisher":"Wiley","issue":"23","license":[{"start":{"date-parts":[[2025,10,28]],"date-time":"2025-10-28T00:00:00Z","timestamp":1761609600000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"funder":[{"DOI":"10.13039\/501100005363","name":"University of Buenos Aires","doi-asserted-by":"publisher","award":["UBACYT 20020190100242BA,20020220300118BA"],"award-info":[{"award-number":["UBACYT 20020190100242BA,20020220300118BA"]}],"id":[{"id":"10.13039\/501100005363","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100002923","name":"Consejo Nacional de Investigaciones Cient\u00edficas y T\u00e9cnicas","doi-asserted-by":"publisher","award":["PIP 11220170100420CO"],"award-info":[{"award-number":["PIP 11220170100420CO"]}],"id":[{"id":"10.13039\/501100002923","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["chemistry-europe.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["ChemMedChem"],"published-print":{"date-parts":[[2025,11,28]]},"abstract":"<jats:p>\n                    Minimolide, a sesquiterpene lactone isolated from\n                    <jats:italic>Mikania minima<\/jats:italic>\n                    , has displayed promising activity against\n                    <jats:italic>Trypanosoma cruzi<\/jats:italic>\n                    . The biocatalytic derivatization of minimolide and its analogs via selective acetylation and deacetylation is reported here using commercial lipases under mild and sustainable conditions. Reaction optimization identified\n                    <jats:italic>Rhizomucor miehei<\/jats:italic>\n                    lipase (RMIM) and\n                    <jats:italic>Candida antarctica<\/jats:italic>\n                    lipase B (CAL B) as the most efficient catalysts for acetylation and regioselective deacetylation, respectively. Structural transformations allow the synthesis of heliangolide and elemanolide analogs. The impact of the sesquiterpene lactone scaffold and acylation pattern on anti\u2010\n                    <jats:italic>Trypanosoma cruzi<\/jats:italic>\n                    activity is evaluated in intracellular amastigotes. Compared to the parent compound, acetylated minimolide show enhanced antiparasitic activity (IC\n                    <jats:sub>50<\/jats:sub>\n                    \u2009= \u20091.08 \u00b5M) and a higher selectivity index (SI\u2009= \u200923.21). Likewise, acetylated heliangolide displayed improved selectivity as a result of reduced cytotoxicity. These findings underscore the usefulness of biocatalytic approaches in designing structurally optimized and more selective antitrypanosomal agents derived from natural lactones.\n                  <\/jats:p>","DOI":"10.1002\/cmdc.202500623","type":"journal-article","created":{"date-parts":[[2025,10,29]],"date-time":"2025-10-29T01:58:50Z","timestamp":1761703130000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Sustainable Modification of Minimolide: Influence of Structure and Acylation Pattern on Anti\u2010\n                    <i>Trypanosoma cruzi<\/i>\n                    Activity"],"prefix":"10.1002","volume":"20","author":[{"given":"Orlando G.","family":"Elso","sequence":"first","affiliation":[{"name":"Laboratorio de Biocat\u00e1lisis. Departamento de Qu\u00edmica Org\u00e1nica y UMYMFOR Naturales Universidad de Buenos Aires\u2014CONICET Facultad de Ciencias Exactas Ciudad Universitaria  Pabell\u00f3n 2 piso 3 C1428EGA Buenos Aires Argentina"},{"name":"C\u00e1tedra de Farmacognosia Facultad de Farmacia y Bioqu\u00edmica Universidad de Buenos Aires  Jun\u00edn piso 2 954 C1113AAD Buenos Aires Argentina"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Augusto E.","family":"Bivona","sequence":"additional","affiliation":[{"name":"Instituto de Microbiolog\u00eda y Parasitolog\u00eda M\u00e9dica (IMPaM) Universidad de Buenos Aires\u2014CONICET Facultad de Farmacia y Bioqu\u00edmica  Paraguay 2155 piso12 Buenos Aires Argentina"},{"name":"Instituto de Estudios de la Inmunidad Humoral (IDEHU) Universidad de Buenos Aires\u2014CONICET Facultad de Farmacia y Bioqu\u00edmica  Jun\u00edn 956 piso 4 Buenos Aires Argentina"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Valeria P.","family":"S\u00fclsen","sequence":"additional","affiliation":[{"name":"C\u00e1tedra de Farmacognosia Facultad de Farmacia y Bioqu\u00edmica Universidad de Buenos Aires  Jun\u00edn piso 2 954 C1113AAD Buenos Aires Argentina"},{"name":"Instituto de Qu\u00edmica y Metabolismo del F\u00e1rmaco (IQUIMEFA) Universidad de Buenos Aires\u2014CONICET Facultad de Farmacia y Bioqu\u00edmica  Jun\u00edn 956 piso 2 C1113AAD Buenos Aires Argentina"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2946-4795","authenticated-orcid":false,"given":"Guadalupe Garc\u00eda","family":"Li\u00f1ares","sequence":"additional","affiliation":[{"name":"Laboratorio de Biocat\u00e1lisis. Departamento de Qu\u00edmica Org\u00e1nica y UMYMFOR Naturales Universidad de Buenos Aires\u2014CONICET Facultad de Ciencias Exactas Ciudad Universitaria  Pabell\u00f3n 2 piso 3 C1428EGA Buenos Aires Argentina"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2025,10,28]]},"reference":[{"key":"e_1_2_8_2_1","first-page":"153","volume-title":"Chagas Disease\u2010Basic Investigations and Challenges","author":"Garc\u00eda Li\u00f1ares G.in","year":"2018"},{"key":"e_1_2_8_3_1","doi-asserted-by":"publisher","DOI":"10.1093\/cid\/cir956"},{"key":"e_1_2_8_4_1","unstructured":"W. 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