{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,22]],"date-time":"2025-10-22T10:48:33Z","timestamp":1761130113668,"version":"build-2065373602"},"reference-count":72,"publisher":"MDPI AG","issue":"24","license":[{"start":{"date-parts":[[2023,12,12]],"date-time":"2023-12-12T00:00:00Z","timestamp":1702339200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"National Institute of Allergy and Infectious Diseases","award":["1R41AI120351-01"],"award-info":[{"award-number":["1R41AI120351-01"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["IJMS"],"abstract":"<jats:p>Thiazole and piperazine are two important heterocyclic rings that play a prominent role in nature and have a broad range of applications in agricultural and medicinal chemistry. Herein, we report the parallel synthesis of a library of diverse piperazine-tethered thiazole compounds. The reaction of piperazine with newly generated 4-chloromethyl-2-amino thiazoles led to the desired piperazine thiazole compounds with high purities and good overall yields. Using a variety of commercially available carboxylic acids, the parallel synthesis of a variety of disubstituted 4-(piperazin-1-ylmethyl)thiazol-2-amine derivatives is described. the screening of the compounds led to the identification of antiplasmodial compounds that exhibited interesting antimalarial activity, primarily against the Plasmodium falciparum chloroquine-resistant Dd2 strain. The hit compound 2291-61 demonstrated an antiplasmodial EC50 of 102 nM in the chloroquine-resistant Dd2 strain and a selectivity of over 140.<\/jats:p>","DOI":"10.3390\/ijms242417414","type":"journal-article","created":{"date-parts":[[2023,12,13]],"date-time":"2023-12-13T04:14:42Z","timestamp":1702440882000},"page":"17414","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":3,"title":["Parallel Synthesis of Piperazine Tethered Thiazole Compounds with Antiplasmodial Activity"],"prefix":"10.3390","volume":"24","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-0198-6903","authenticated-orcid":false,"given":"Ramanjaneyulu","family":"Rayala","sequence":"first","affiliation":[{"name":"Herbert Wertheim College of Medicine, Center for Translational Science, Florida International University, Miami, FL 33199, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Prakash","family":"Chaudhari","sequence":"additional","affiliation":[{"name":"Herbert Wertheim College of Medicine, Center for Translational Science, Florida International University, Miami, FL 33199, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0009-0003-3784-5306","authenticated-orcid":false,"given":"Ashley","family":"Bunnell","sequence":"additional","affiliation":[{"name":"Herbert Wertheim College of Medicine, Center for Translational Science, Florida International University, Miami, FL 33199, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Bracken","family":"Roberts","sequence":"additional","affiliation":[{"name":"Division of Molecular Microbiology, Burnett School of Biomedical Sciences, University of Central Florida, Orlando, FL 32826, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Debopam","family":"Chakrabarti","sequence":"additional","affiliation":[{"name":"Division of Molecular Microbiology, Burnett School of Biomedical Sciences, University of Central Florida, Orlando, FL 32826, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Adel","family":"Nefzi","sequence":"additional","affiliation":[{"name":"Herbert Wertheim College of Medicine, Center for Translational Science, Florida International University, Miami, FL 33199, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2023,12,12]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"345","DOI":"10.1021\/cc700187t","article-title":"Application of combinatorial chemistry science on modern drug discovery","volume":"10","author":"Kennedy","year":"2008","journal-title":"J. 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