{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,2,28]],"date-time":"2026-02-28T10:52:14Z","timestamp":1772275934087,"version":"3.50.1"},"reference-count":39,"publisher":"MDPI AG","issue":"10","license":[{"start":{"date-parts":[[2022,9,20]],"date-time":"2022-09-20T00:00:00Z","timestamp":1663632000000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"NFKI","award":["K-132685"],"award-info":[{"award-number":["K-132685"]}]},{"name":"NFKI","award":["TKP2020-IKA-04"],"award-info":[{"award-number":["TKP2020-IKA-04"]}]},{"name":"Ministry for Innovation and Technology in Hungary","award":["K-132685"],"award-info":[{"award-number":["K-132685"]}]},{"name":"Ministry for Innovation and Technology in Hungary","award":["TKP2020-IKA-04"],"award-info":[{"award-number":["TKP2020-IKA-04"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["JoF"],"abstract":"<jats:p>As the recent outbreak of coronavirus disease 2019 (COVID-19) has shown, viral infections are prone to secondary complications like invasive aspergillosis with a high mortality rate, and therefore the development of novel, effective antifungals is of paramount importance. We have previously demonstrated that 1-amino-5-isocyanonaphthalene (ICAN) derivatives are promising original drug candidates against Candida strains (Patent pending), even against fluconazole resistant C. albicans. Consequently, in this study ICANs were tested on Aspergillus fumigatus, an opportunistic pathogen, which is the leading cause of invasive and systematic pulmonary aspergillosis in immunosuppressed, transplanted and cancer- or COVID-19 treated patients. We have tested several N-alkylated ICANs, a well as 1,5-naphthalene-diisocyanide (DIN) with the microdilution method against Aspergillus fumigatus strains. The results revealed that the diisocyanide (DIN) was the most effective with a minimum inhibitory concentration (MIC) value as low as 0.6 \u00b5g mL\u22121 (3.4 \u00b5M); however, its practical applicability is limited by its poor water solubility, which needs to be overcome by proper formulation. The other alkylated derivatives also have in vitro and in vivo anti-Aspergillus fumigatus effects. For animal experiments the second most effective derivative 1-N, N-dimethylamino-5-isocyanonaphthalene (DIMICAN, MIC: 7\u20138 \u00b5g mL\u22121, 36\u201341 \u00b5M) was selected, toxicity tests were made with mice, and then the antifungal effect of DIMICAN was tested in a neutropenic aspergillosis murine model. Compared to amphotericin B (AMB), a well-known antifungal, the antifungal effect of DIMICAN in vivo turned out to be much better (40% vs. 90% survival after eight days), indicating its potential as a clinical drug candidate.<\/jats:p>","DOI":"10.3390\/jof8100985","type":"journal-article","created":{"date-parts":[[2022,9,20]],"date-time":"2022-09-20T22:36:44Z","timestamp":1663713404000},"page":"985","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":5,"title":["Potential Original Drug for Aspergillosis: In Vitro and In Vivo Effects of 1-N,N-Dimethylamino-5-Isocyanonaphthalene (DIMICAN) on Aspergillus fumigatus"],"prefix":"10.3390","volume":"8","author":[{"given":"Zsuzsa M\u00e1th\u00e9n\u00e9","family":"Szigeti","sequence":"first","affiliation":[{"name":"Department of Molecular Biotechnology and Microbiology, Faculty of Science, University of Debrecen, 4010 Debrecen, Hungary"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"L\u00e1szl\u00f3","family":"T\u00e1las","sequence":"additional","affiliation":[{"name":"Department of Molecular Biotechnology and Microbiology, Faculty of Science, University of Debrecen, 4010 Debrecen, Hungary"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4101-3177","authenticated-orcid":false,"given":"Adrienn","family":"Sz\u00e9les","sequence":"additional","affiliation":[{"name":"Department of Lang Utilisation, Engineering and Precision Farming Technology, Faculty of Agricultural and Food Sciences and Environmental Management, University of Debrecen, B\u00f6sz\u00f6rm\u00e9nyi 138, 4032 Debrecen, Hungary"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Zolt\u00e1n","family":"Hargitai","sequence":"additional","affiliation":[{"name":"Department of Pathology, Faculty of General Medicine, University of Debrecen, 4031 Debrecen, Hungary"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Zsolt L\u00e1szl\u00f3","family":"Nagy","sequence":"additional","affiliation":[{"name":"Department of Applied Chemistry, Faculty of Science, University of Debrecen, 4010 Debrecen, Hungary"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-3484-2244","authenticated-orcid":false,"given":"Mikl\u00f3s","family":"Nagy","sequence":"additional","affiliation":[{"name":"Institute of Chemistry, University of Miskolc, Miskolc-Egyetemv\u00e1ros, 3515 Miskolc, Hungary"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Alexandra","family":"Kiss","sequence":"additional","affiliation":[{"name":"Department of Molecular Biotechnology and Microbiology, Faculty of Science, University of Debrecen, 4010 Debrecen, Hungary"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5274-6117","authenticated-orcid":false,"given":"S\u00e1ndor","family":"K\u00e9ki","sequence":"additional","affiliation":[{"name":"Department of Applied Chemistry, Faculty of Science, University of Debrecen, 4010 Debrecen, Hungary"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"G\u00e1bor","family":"Szem\u00e1n-Nagy","sequence":"additional","affiliation":[{"name":"Department of Molecular Biotechnology and Microbiology, Faculty of Science, University of Debrecen, 4010 Debrecen, Hungary"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2022,9,20]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"310","DOI":"10.1128\/CMR.12.2.310","article-title":"Aspergillus fumigatus and aspergillosis","volume":"12","author":"Latge","year":"1999","journal-title":"Clin. 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