{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,12]],"date-time":"2026-10-12T18:46:55Z","timestamp":1791830815755,"version":"4.3.4"},"reference-count":43,"publisher":"MDPI AG","issue":"6","license":[{"start":{"date-parts":[[2024,6,3]],"date-time":"2024-06-03T00:00:00Z","timestamp":1717372800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100006769","name":"Russian Science Foundation","doi-asserted-by":"publisher","award":["22-24-00756"],"award-info":[{"award-number":["22-24-00756"]}],"id":[{"id":"10.13039\/501100006769","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100006769","name":"Russian Science Foundation","doi-asserted-by":"publisher","award":["24-14-00081"],"award-info":[{"award-number":["24-14-00081"]}],"id":[{"id":"10.13039\/501100006769","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100006769","name":"Russian Science Foundation","doi-asserted-by":"publisher","award":["24-14-00090"],"award-info":[{"award-number":["24-14-00090"]}],"id":[{"id":"10.13039\/501100006769","id-type":"DOI","asserted-by":"publisher"}]},{"name":"Ministry of Science and Higher Education","award":["22-24-00756"],"award-info":[{"award-number":["22-24-00756"]}]},{"name":"Ministry of Science and Higher Education","award":["24-14-00081"],"award-info":[{"award-number":["24-14-00081"]}]},{"name":"Ministry of Science and Higher Education","award":["24-14-00090"],"award-info":[{"award-number":["24-14-00090"]}]},{"name":"Arab Republic of Egypt","award":["22-24-00756"],"award-info":[{"award-number":["22-24-00756"]}]},{"name":"Arab Republic of Egypt","award":["24-14-00081"],"award-info":[{"award-number":["24-14-00081"]}]},{"name":"Arab Republic of Egypt","award":["24-14-00090"],"award-info":[{"award-number":["24-14-00090"]}]},{"name":"Russian Federation","award":["22-24-00756"],"award-info":[{"award-number":["22-24-00756"]}]},{"name":"Russian Federation","award":["24-14-00081"],"award-info":[{"award-number":["24-14-00081"]}]},{"name":"Russian Federation","award":["24-14-00090"],"award-info":[{"award-number":["24-14-00090"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceuticals"],"abstract":"<jats:p>A series of hybrid compounds with triazole and thiazolidine nuclei connected by a linker has been synthesized and extensively studied. Various synthetic methods for the target compounds have been tested. A microbiological assessment of the obtained compounds was carried out on strains of pathogenic fungi C. albicans, C. non-albicans, multidrug-resistant C. auris, Rhizopus arrhizus, Aspergillus spp. and some dermatophytes and other yeasts. The lowest obtained MIC values for target compounds lie between 0.003 \u00b5g\/mL and 0.5 \u00b5g\/mL and therefore the compounds are not inferior or several times better than commercial azole drugs. The length of the acylpiperazine linker has a limited effect on antifungal activity. Some bioisosteric analogues were tested in microbiological analysis, but turned out to be weaker than the leader in activity. The highest activity was demonstrated by a compound with para-chlorobenzylidene substituent in the thiazolidine fragment. Molecular modelling was used to predict binding modes of synthesized molecules and rationalize experimentally observed SAR. The leader compound is twice more effective in inhibiting the formation of germ tubes by Candida albicans yeast cells compared to voriconazole. An increased level of Pdr5, an azoles drug efflux pump was observed, but the increase is lower than that caused by azoles. The results can be useful for further development of more powerful and safe antifungal agents.<\/jats:p>","DOI":"10.3390\/ph17060723","type":"journal-article","created":{"date-parts":[[2024,6,3]],"date-time":"2024-06-03T10:08:38Z","timestamp":1717409318000},"page":"723","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":7,"title":["Synthesis and Biological Evaluation of a Series of New Hybrid Amide Derivatives of Triazole and Thiazolidine-2,4-dione"],"prefix":"10.3390","volume":"17","author":[{"given":"Igor B.","family":"Levshin","sequence":"first","affiliation":[{"name":"Gause Institute of New Antibiotics, 11 B. Pirogovskaya Street, 119021 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Alexander Yu.","family":"Simonov","sequence":"additional","affiliation":[{"name":"Gause Institute of New Antibiotics, 11 B. Pirogovskaya Street, 119021 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Alexey A.","family":"Panov","sequence":"additional","affiliation":[{"name":"Gause Institute of New Antibiotics, 11 B. Pirogovskaya Street, 119021 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Natalia E.","family":"Grammatikova","sequence":"additional","affiliation":[{"name":"Gause Institute of New Antibiotics, 11 B. Pirogovskaya Street, 119021 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7250-4740","authenticated-orcid":false,"given":"Alexander I.","family":"Alexandrov","sequence":"additional","affiliation":[{"name":"Bach Institute of Biochemistry, Federal Research Center of Biotechnology of the RAS, 119071 Moscow, Russia"},{"name":"Institute of Biochemical Technology and Nanotechnology, Peoples\u2019 Friendship University of Russia (RUDN), 6 Miklukho-Maklaya Street, 17198 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Eslam S. M. O.","family":"Ghazy","sequence":"additional","affiliation":[{"name":"Bach Institute of Biochemistry, Federal Research Center of Biotechnology of the RAS, 119071 Moscow, Russia"},{"name":"Institute of Biochemical Technology and Nanotechnology, Peoples\u2019 Friendship University of Russia (RUDN), 6 Miklukho-Maklaya Street, 17198 Moscow, Russia"},{"name":"Department of Microbiology, Faculty of Pharmacy, Tanta University, Tanta 31111, Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9664-9506","authenticated-orcid":false,"given":"Vasiliy A.","family":"Ivlev","sequence":"additional","affiliation":[{"name":"Institute of Biochemical Technology and Nanotechnology, Peoples\u2019 Friendship University of Russia (RUDN), 6 Miklukho-Maklaya Street, 17198 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9270-9476","authenticated-orcid":false,"given":"Michael O.","family":"Agaphonov","sequence":"additional","affiliation":[{"name":"Bach Institute of Biochemistry, Federal Research Center of Biotechnology of the RAS, 119071 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Alexey B.","family":"Mantsyzov","sequence":"additional","affiliation":[{"name":"Faculty of Fundamental Medicine, Lomonosov Moscow State University, 27\/1 Lomonosovsky Ave., 119991 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-3216-5737","authenticated-orcid":false,"given":"Vladimir I.","family":"Polshakov","sequence":"additional","affiliation":[{"name":"Faculty of Fundamental Medicine, Lomonosov Moscow State University, 27\/1 Lomonosovsky Ave., 119991 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2024,6,3]]},"reference":[{"key":"ref_1","unstructured":"WHO (2024, May 29). 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