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Pyrazolo[1,5\u2010<jats:italic>a<\/jats:italic>]pyrimidine motifs were synthesized via the reaction of aminopyrazole derivative <jats:bold>9<\/jats:bold> with some electrophilic reagents and systematically characterized. The antimicrobial potential of these molecules was assessed against <jats:styled-content style=\"fixed-case\"><jats:italic>Staphylococcus aureus<\/jats:italic><\/jats:styled-content>, <jats:styled-content style=\"fixed-case\"><jats:italic>Escherichia coli<\/jats:italic><\/jats:styled-content>, and <jats:styled-content style=\"fixed-case\"><jats:italic>Candida albicans<\/jats:italic><\/jats:styled-content>. Among the tested derivatives, compounds <jats:bold>6<\/jats:bold>, <jats:bold>20<\/jats:bold>, and <jats:bold>22<\/jats:bold> emerged as particularly effective, with minimum inhibitory concentrations (MICs) reaching as low as 3.125\u2009\u03bcg\/mL. Structure\u2013activity relationship (SAR) analysis highlighted the role of electron\u2010withdrawing groups in enhancing bioactivity. Molecular docking studies further supported the experimental findings, showing favorable interactions with bacterial DNA gyrase (PDB ID: 1KZN). Additionally, SwissADME profiling revealed that the compounds possess promising drug\u2010like properties and oral bioavailability. These findings position the synthesized thiazole\u2010containing scaffolds as promising candidates for future antimicrobial drug development.<\/jats:p>","DOI":"10.1111\/cbdd.70124","type":"journal-article","created":{"date-parts":[[2025,5,21]],"date-time":"2025-05-21T08:19:15Z","timestamp":1747815555000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":7,"title":["Exploring Thiazole\u2010Based Heterocycles: Synthesis, Bioactivity, and Molecular Docking for Antimicrobial Applications"],"prefix":"10.1111","volume":"105","author":[{"given":"Hana M.","family":"Abumelha","sequence":"first","affiliation":[{"name":"Department of Chemistry, College of Science Princess Nourah Bint Abdulrahman University  Riyadh Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Fatmah O.","family":"Sefrji","sequence":"additional","affiliation":[{"name":"Department of Biology, College of Science Taibah University  Al\u2010Madinah Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0804-2339","authenticated-orcid":false,"given":"Abdulmajeed F.","family":"Alrefaei","sequence":"additional","affiliation":[{"name":"Department of Biology\/Genetic and Molecular Biology Central Laboratory (GMCL) Jamoum University College, Umm Al\u2010Qura University  Makkah Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mariam","family":"Mojally","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Science, Faculty of Pharmacy Umm Al\u2010Qura University  Makkah Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Fatimah A.","family":"Alotaibi","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Science, University of Tabuk  Tabuk Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Khadra B.","family":"Alomari","sequence":"additional","affiliation":[{"name":"Department of Physical Sciences, Chemistry Division, College of Science Jazan University  Jazan Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Fatimah M.","family":"Madkhaly","sequence":"additional","affiliation":[{"name":"Department of Basic Medical Sciences (Pathology), Faculty of Medicine Jazan University  Jazan Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-0619-6206","authenticated-orcid":false,"given":"Nashwa M.","family":"El\u2010Metwaly","sequence":"additional","affiliation":[{"name":"Department of Chemistry, College of Science Umm Al\u2010Qura University  Makkah Saudi Arabia"},{"name":"Department of Chemistry, Faculty of Science Mansoura University  Mansoura Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2025,5,21]]},"reference":[{"key":"e_1_2_10_2_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2017.07.007"},{"key":"e_1_2_10_3_1","doi-asserted-by":"publisher","DOI":"10.1002\/ardp.200500259"},{"key":"e_1_2_10_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.saa.2011.12.054"},{"key":"e_1_2_10_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2010.01.029"},{"key":"e_1_2_10_6_1","doi-asserted-by":"publisher","DOI":"10.3390\/molecules29102232"},{"key":"e_1_2_10_7_1","doi-asserted-by":"publisher","DOI":"10.3390\/80200275"},{"key":"e_1_2_10_8_1","doi-asserted-by":"publisher","DOI":"10.1002\/jhet.5570380430"},{"key":"e_1_2_10_9_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2007.12.019"},{"key":"e_1_2_10_10_1","doi-asserted-by":"publisher","DOI":"10.1021\/jf035233z"},{"key":"e_1_2_10_11_1","doi-asserted-by":"publisher","DOI":"10.1111\/jphp.13331"},{"key":"e_1_2_10_12_1","doi-asserted-by":"publisher","DOI":"10.3389\/fmolb.2023.1112521"},{"key":"e_1_2_10_13_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmc.2013.07.027"},{"key":"e_1_2_10_14_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmc.2017.10.012"},{"key":"e_1_2_10_15_1","doi-asserted-by":"publisher","DOI":"10.2174\/1568026616666160506130731"},{"key":"e_1_2_10_16_1","doi-asserted-by":"publisher","DOI":"10.1002\/jhet.5570380329"},{"key":"e_1_2_10_17_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2008.04.001"},{"key":"e_1_2_10_18_1","doi-asserted-by":"publisher","DOI":"10.5567\/pharmacologia.2014.1.11"},{"key":"e_1_2_10_19_1","first-page":"1","article-title":"Enaminonitriles in Heterocyclic Synthesis: Synthesis and Biological Evaluation of Novel Indeno[2,1\u2010b]Thiophene Derivatives","volume":"37","author":"Fadda A. 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