{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,2]],"date-time":"2026-10-02T23:22:24Z","timestamp":1790983344403,"version":"4.1.0"},"reference-count":115,"publisher":"MDPI AG","issue":"20","license":[{"start":{"date-parts":[[2022,10,19]],"date-time":"2022-10-19T00:00:00Z","timestamp":1666137600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Chalcones have been well examined in the extant literature and demonstrated antibacterial, antifungal, anti-inflammatory, and anticancer properties. A detailed evaluation of the purported health benefits of chalcone and its derivatives, including molecular mechanisms of pharmacological activities, can be further explored. Therefore, this review aimed to describe the main characteristics of chalcone and its derivatives, including their method synthesis and pharmacotherapeutics applications with molecular mechanisms. The presence of the reactive \u03b1,\u03b2-unsaturated system in the chalcone\u2019s rings showed different potential pharmacological properties, including inhibitory activity on enzymes, anticancer, anti-inflammatory, antibacterial, antifungal, antimalarial, antiprotozoal, and anti-filarial activity. Changing the structure by adding substituent groups to the aromatic ring can increase potency, reduce toxicity, and broaden pharmacological action. This report also summarized the potential health benefits of chalcone derivatives, particularly antimicrobial activity. We found that several chalcone compounds can inhibit diverse targets of antibiotic-resistance development pathways; therefore, they overcome resistance, and bacteria become susceptible to antibacterial compounds. A few chalcone compounds were more active than conventional antibiotics, like vancomycin and tetracycline. On another note, a series of pyran-fused chalcones and trichalcones can block the NF-B signaling complement system implicated in inflammation, and several compounds demonstrated more potent lipoxygenase inhibition than NSAIDs, such as indomethacin. This report integrated discussion from the domains of medicinal chemistry, organic synthesis, and diverse pharmacological applications, particularly for the development of new anti-infective agents that could be a useful reference for pharmaceutical scientists.<\/jats:p>","DOI":"10.3390\/molecules27207062","type":"journal-article","created":{"date-parts":[[2022,10,19]],"date-time":"2022-10-19T22:19:53Z","timestamp":1666217993000},"page":"7062","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":134,"title":["Pharmacotherapeutics Applications and Chemistry of Chalcone Derivatives"],"prefix":"10.3390","volume":"27","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-3357-388X","authenticated-orcid":false,"given":"Jagjit Singh","family":"Dhaliwal","sequence":"first","affiliation":[{"name":"PAPRSB Institute of Health Sciences, Universiti Brunei Darussalam, Gadong BE1410, Brunei"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4840-0460","authenticated-orcid":false,"given":"Said","family":"Moshawih","sequence":"additional","affiliation":[{"name":"PAPRSB Institute of Health Sciences, Universiti Brunei Darussalam, Gadong BE1410, Brunei"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-6686-7019","authenticated-orcid":false,"given":"Khang Wen","family":"Goh","sequence":"additional","affiliation":[{"name":"Faculty of Data Science and Information Technology, INTI International University, Nilai 71800, Malaysia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mei Jun","family":"Loy","sequence":"additional","affiliation":[{"name":"Faculty of Engineering, Universiti Teknologi Malaysia, Skudai 81300, Malaysia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5686-2943","authenticated-orcid":false,"given":"Md. Sanower","family":"Hossain","sequence":"additional","affiliation":[{"name":"Centre for Sustainability of Ecosystem and Earth Resources (Pusat ALAM), Universiti Malaysia Pahang, Kuantan 26300, Malaysia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9716-3126","authenticated-orcid":false,"given":"Andi","family":"Hermansyah","sequence":"additional","affiliation":[{"name":"Department of Pharmacy Practice, Faculty of Pharmacy, Universitas Airlangga, Surabaya 60115, Indonesia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2043-4928","authenticated-orcid":false,"given":"Vijay","family":"Kotra","sequence":"additional","affiliation":[{"name":"Faculty of Pharmacy, Quest International University, Ipoh 30250, Malaysia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8817-7956","authenticated-orcid":false,"given":"Nurolaini","family":"Kifli","sequence":"additional","affiliation":[{"name":"PAPRSB Institute of Health Sciences, Universiti Brunei Darussalam, Gadong BE1410, Brunei"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-0480-399X","authenticated-orcid":false,"given":"Hui Poh","family":"Goh","sequence":"additional","affiliation":[{"name":"PAPRSB Institute of Health Sciences, Universiti Brunei Darussalam, Gadong BE1410, Brunei"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sachinjeet Kaur Sodhi","family":"Dhaliwal","sequence":"additional","affiliation":[{"name":"PAPRSB Institute of Health Sciences, Universiti Brunei Darussalam, Gadong BE1410, Brunei"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hayati","family":"Yassin","sequence":"additional","affiliation":[{"name":"Faculty of Integrated Technologies, Universiti Brunei Darussalam, Gadong BE1410, Brunei"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6971-1383","authenticated-orcid":false,"given":"Long Chiau","family":"Ming","sequence":"additional","affiliation":[{"name":"PAPRSB Institute of Health Sciences, Universiti Brunei Darussalam, Gadong BE1410, Brunei"},{"name":"Department of Pharmacy Practice, Faculty of Pharmacy, Universitas Airlangga, Surabaya 60115, Indonesia"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2022,10,19]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"351","DOI":"10.1517\/13543776.2014.995627","article-title":"Potential pharmacological uses of chalcones: A patent review (from June 2011\u20132014)","volume":"25","author":"Matos","year":"2015","journal-title":"Expert Opin. 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