{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,11,2]],"date-time":"2025-11-02T06:32:11Z","timestamp":1762065131601,"version":"build-2065373602"},"reference-count":33,"publisher":"MDPI AG","issue":"17","license":[{"start":{"date-parts":[[2022,8,25]],"date-time":"2022-08-25T00:00:00Z","timestamp":1661385600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"NIH NIAID","award":["R01AI165473"],"award-info":[{"award-number":["R01AI165473"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["IJMS"],"abstract":"<jats:p>COVID-19, caused by the highly transmissible severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), has rapidly spread and become a pandemic since its outbreak in 2019. We have previously discovered that aloperine is a new privileged scaffold that can be modified to become a specific antiviral compound with markedly improved potency against different viruses, such as the influenza virus. In this study, we have identified a collection of aloperine derivatives that can inhibit the entry of SARS-CoV-2 into host cells. Compound 5 is the most potent tested aloperine derivative that inhibited the entry of SARS-CoV-2 (D614G variant) spike protein-pseudotyped virus with an IC50 of 0.5 \u00b5M. The compound was also active against several other SARS-CoV-2 variants including Delta and Omicron. Results of a confocal microscopy study suggest that compound 5 inhibited the viral entry before fusion to the cell or endosomal membrane. The results are consistent with the notion that aloperine is a privileged scaffold that can be used to develop potent anti-SARS-CoV-2 entry inhibitors.<\/jats:p>","DOI":"10.3390\/ijms23179659","type":"journal-article","created":{"date-parts":[[2022,8,26]],"date-time":"2022-08-26T02:04:32Z","timestamp":1661479472000},"page":"9659","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":6,"title":["Quinolizidines as Novel SARS-CoV-2 Entry Inhibitors"],"prefix":"10.3390","volume":"23","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-5659-4053","authenticated-orcid":false,"given":"Li","family":"Huang","sequence":"first","affiliation":[{"name":"Department of Surgery, Duke University Medical Center, Durham, NC 27710, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Lei","family":"Zhu","sequence":"additional","affiliation":[{"name":"Department of Surgery, Duke University Medical Center, Durham, NC 27710, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Hua","family":"Xie","sequence":"additional","affiliation":[{"name":"School of Dentistry, Meharry Medical College, Nashville, TN 37208, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jeffery Shawn","family":"Goodwin","sequence":"additional","affiliation":[{"name":"Department of Biochemistry and Cancer Biology, Meharry Medical College, Nashville, TN 37208, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Tanu","family":"Rana","sequence":"additional","affiliation":[{"name":"Department of Biochemistry and Cancer Biology, Meharry Medical College, Nashville, TN 37208, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Lan","family":"Xie","sequence":"additional","affiliation":[{"name":"Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-6880-2104","authenticated-orcid":false,"given":"Chin-Ho","family":"Chen","sequence":"additional","affiliation":[{"name":"Department of Surgery, Duke University Medical Center, Durham, NC 27710, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2022,8,25]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"192","DOI":"10.1111\/joim.13091","article-title":"COVID-19 diagnosis and management: A comprehensive review","volume":"288","author":"Pascarella","year":"2020","journal-title":"J. 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