{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,6,25]],"date-time":"2026-06-25T11:37:12Z","timestamp":1782387432801,"version":"3.54.5"},"reference-count":28,"publisher":"American Society for Microbiology","issue":"8","license":[{"start":{"date-parts":[[2017,8,1]],"date-time":"2017-08-01T00:00:00Z","timestamp":1501545600000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.asm.org\/non-commercial-tdm-license"}],"content-domain":{"domain":["journals.asm.org"],"crossmark-restriction":true},"short-container-title":["Antimicrob Agents Chemother"],"published-print":{"date-parts":[[2017,8]]},"abstract":"<jats:title>ABSTRACT<\/jats:title>\n          <jats:p>\n            Despite recent advances in diagnostic and therapeutic methods in antifungal research, aspergillosis still remains a leading cause of morbidity and mortality. One strategy to address this problem is to enhance the activity spectrum of known antifungals, and we now report the first successful application of\n            <jats:named-content content-type=\"genus-species\">Candida antarctica<\/jats:named-content>\n            lipase (CAL) for the preparation of optically enriched fluconazole analogues. Anti-\n            <jats:named-content content-type=\"genus-species\">Aspergillus<\/jats:named-content>\n            activity was observed for an optically enriched derivative, (\u2212)-\n            <jats:italic>S<\/jats:italic>\n            -2-(2\u2032,4\u2032-difluorophenyl)-1-hexyl-amino-3-(1\u2034,2\u2034,4\u2034)triazol-1\u2034-yl-propan-2-ol, which exhibits MIC values of 15.6 \u03bcg\/ml and 7.8 \u03bcg\/disc in broth microdilution and disc diffusion assays, respectively. This compound is tolerated by mammalian erythrocytes and cell lines (A549 and U87) at concentrations of up to 1,000 \u03bcg\/ml. When incorporated into dextran nanoparticles, the novel, optically enriched fluconazole analogue exhibited improved antifungal activity against\n            <jats:named-content content-type=\"genus-species\">Aspergillus fumigatus<\/jats:named-content>\n            (MIC, 1.63 \u03bcg\/ml). These results not only demonstrate the ability of biocatalytic approaches to yield novel, optically enriched fluconazole derivatives but also suggest that enantiomerically pure fluconazole derivatives, and their nanotized counterparts, exhibiting anti-\n            <jats:named-content content-type=\"genus-species\">Aspergillus<\/jats:named-content>\n            activity may have reduced toxicity.\n          <\/jats:p>","DOI":"10.1128\/aac.00273-17","type":"journal-article","created":{"date-parts":[[2017,6,13]],"date-time":"2017-06-13T00:30:23Z","timestamp":1497313823000},"update-policy":"https:\/\/doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":6,"title":["Chemoenzymatic Synthesis, Nanotization, and Anti-Aspergillus Activity of Optically Enriched Fluconazole Analogues"],"prefix":"10.1128","volume":"61","author":[{"given":"Shashwat","family":"Malhotra","sequence":"first","affiliation":[{"name":"Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi, India"},{"name":"Kirori Mal College, Department of Chemistry, University of Delhi, Delhi, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Seema","family":"Singh","sequence":"additional","affiliation":[{"name":"CSIR-Institute of Genomics and Integrative Biology, Delhi, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Neha","family":"Rana","sequence":"additional","affiliation":[{"name":"Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shilpi","family":"Tomar","sequence":"additional","affiliation":[{"name":"Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Priyanka","family":"Bhatnagar","sequence":"additional","affiliation":[{"name":"CSIR-Institute of Genomics and Integrative Biology, Delhi, 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