Screened antipsychotic drugs inhibit SARS-CoV-2 binding with ACE2 in vitro was written by Lu, Jiayu;Hou, Yajing;Ge, Shuai;Wang, Xiangjun;Wang, Jue;Hu, Tian;Lv, Yuexin;He, Huaizhen;Wang, Cheng. And the article was included in Life Sciences in 2021.HPLC of Formula: 50-52-2 This article mentions the following:
The coronavirus disease 2019 (COVID-19) pandemic has swept the globe and no specific effective drug has been identified. Drug repurposing is a well-known method to address the crisis in a time-critical fashion. Antipsychotic drugs (APDs) have been reported to inhibit DNA replication of hepatitis B virus, measles virus germination, and HIV infection, along with replication of SARS-CoV and MERS-CoV, both of which interact with host cells as SARS-CoV-2. Nineteen APDs were screened using ACE2-HEK293T cell membrane chromatog. (ACE2-HEK293T/CMC). Cytotoxicity assay, coronavirus spike pseudotype virus entry assay, surface plasmon resonance, and virtual mol. docking were applied to detect affinity between ACE2 protein and drugs and a potential antiviral property of the screened compounds After the CMC screening, 8 of the 19 APDs were well-retained on ACE2-HEK293T/CMC column and showed significant antiviral activities in vitro. Three quarters of them belong to phenothiazine and could significantly inhibit the entrance of coronavirus into ACE2-HEK293T cells. Two other drugs, aripiprazole and tiapride, exhibited weaker inhibition. We selected 5 of the drugs for subsequent evaluation. All 5 showed similar affinity to ACE2 and virtual mol. docking demonstrated they bound with different amino acids resp. on ACE2 which SARS-CoV-2 binds to. Eight APDs were screened for binding with ACE2, 5 of which demonstrated potential protective effects against SARS-CoV-2 through acting on ACE2. Although the 5 drugs have a weak ability to block SARS-CoV-2 with a single binding site, they may provide a synergistic effect in adjuvant therapy of COVID-19 infection. In the experiment, the researchers used many compounds, for example, 10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2HPLC of Formula: 50-52-2).
10-(2-(1-Methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine (cas: 50-52-2) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.HPLC of Formula: 50-52-2
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem