{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,10]],"date-time":"2026-10-10T13:23:07Z","timestamp":1791638587949,"version":"4.3.4"},"reference-count":85,"publisher":"MDPI AG","issue":"11","license":[{"start":{"date-parts":[[2021,10,28]],"date-time":"2021-10-28T00:00:00Z","timestamp":1635379200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Serbian Ministry of Education, Science and Technological Development","award":["451-03-9\/2021-14\/200007"],"award-info":[{"award-number":["451-03-9\/2021-14\/200007"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceuticals"],"abstract":"<jats:p>This manuscript deals with the synthesis and computational and experimental evaluation of the antimicrobial activity of twenty-nine 4-(indol-3-yl)thiazole-2-amines and 4-\u03b9ndol-3-yl)thiazole acylamines. An evaluation of antibacterial activity against Gram (+) and Gram (\u2212) bacteria revealed that the MIC of indole derivatives is in the range of 0.06\u20131.88 mg\/mL, while among fourteen methylindole derivatives, only six were active, with an MIC in the range of of 0.47\u20131.88 mg\/mL. S. aureus appeared to be the most resistant strain, while S. Typhimurium was the most sensitive. Compound 5x was the most promising, with an MIC in the range of 0.06\u20130.12 mg\/mL, followed by 5d and 5m. An evaluation of these three compounds against resistant strains, namely MRSA P.\u00a0aeruginosa and E.\u00a0coli, revealed that they were more potent against MRSA than ampicillin. Furthermore, compounds 5m and 5x were superior inhibitors of biofilm formation, compared to ampicillin and streptomycin, in terms Compounds 5d, 5m, and 5x interact with streptomycin in additive manner. The antifungal activity of some compounds exceeded or was equipotent to those of the reference antifungal agents bifonazole and ketoconazole. The most potent antifungal agent was found to be compound 5g. Drug likeness scores of compounds was in a range of \u22120.63 to 0.29, which is moderate to good. According to docking studies, E. coli MurB inhibition is probably responsible for the antibacterial activity of compounds, whereas CYP51 inhibition was implicated in antifungal activity. Compounds appeared to be non-toxic, according to the cytotoxicity assessment in MRC-5 cells.<\/jats:p>","DOI":"10.3390\/ph14111096","type":"journal-article","created":{"date-parts":[[2021,10,28]],"date-time":"2021-10-28T23:51:36Z","timestamp":1635465096000},"page":"1096","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":22,"title":["4-(Indol-3-yl)thiazole-2-amines and 4-\u03b9ndol-3-yl)thiazole Acylamines as \u039dovel Antimicrobial Agents: Synthesis, In Silico and In Vitro Evaluation"],"prefix":"10.3390","volume":"14","author":[{"given":"Sergei","family":"Simakov","sequence":"first","affiliation":[{"name":"Laboratory of General Chemistry, Chemistry Department, Belgorod State University, 308015 Belgorod, Belgorod Oblast, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Victor","family":"Kartsev","sequence":"additional","affiliation":[{"name":"InterBioScreen, 142432 Chernogolovka, Moscow Region, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8587-2710","authenticated-orcid":false,"given":"Anthi","family":"Petrou","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ioannis","family":"Nicolaou","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9894-7777","authenticated-orcid":false,"given":"Athina","family":"Geronikaki","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2480-5490","authenticated-orcid":false,"given":"Marija","family":"Ivanov","sequence":"additional","affiliation":[{"name":"Mycological Laboratory, Department of Plant Physiology, Institute for Biological Research \u201cSini\u0161a Stankovi\u0107\u201d, National Institute of Republic of Serbia, University of Belgrade, 11060 Beograd, Serbia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Marina","family":"Kostic","sequence":"additional","affiliation":[{"name":"Mycological Laboratory, Department of Plant Physiology, Institute for Biological Research \u201cSini\u0161a Stankovi\u0107\u201d, National Institute of Republic of Serbia, University of Belgrade, 11060 Beograd, Serbia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-6823-1137","authenticated-orcid":false,"given":"Jasmina","family":"Glamo\u010dlija","sequence":"additional","affiliation":[{"name":"Mycological Laboratory, Department of Plant Physiology, Institute for Biological Research \u201cSini\u0161a Stankovi\u0107\u201d, National Institute of Republic of Serbia, University of Belgrade, 11060 Beograd, Serbia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7381-756X","authenticated-orcid":false,"given":"Marina","family":"Sokovi\u0107","sequence":"additional","affiliation":[{"name":"Mycological Laboratory, Department of Plant Physiology, Institute for Biological Research \u201cSini\u0161a Stankovi\u0107\u201d, National Institute of Republic of Serbia, University of Belgrade, 11060 Beograd, Serbia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Despoina","family":"Talea","sequence":"additional","affiliation":[{"name":"Laboratory of Pharmacology, School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1459-9774","authenticated-orcid":false,"given":"Ioannis S.","family":"Vizirianakis","sequence":"additional","affiliation":[{"name":"Laboratory of Pharmacology, School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece"},{"name":"Department of Life and Health Sciences, University of Nicosia, Nicosia CY-1700, Cyprus"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2021,10,28]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"417","DOI":"10.1128\/MMBR.00016-10","article-title":"Origins and evolution of antibiotic resistance","volume":"74","author":"Davies","year":"2010","journal-title":"Microbiol Mol. 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