A simple and efficient procedure for the synthesis of substituted benzothiazoles through condensation of 2-aminothiophenol with aromatic aldehydes in the presence of H2O2/HCl system in ethanol at room temperature is d...A simple and efficient procedure for the synthesis of substituted benzothiazoles through condensation of 2-aminothiophenol with aromatic aldehydes in the presence of H2O2/HCl system in ethanol at room temperature is described. The target compounds have been characterized by ^1H NMR, ^13C NMR, IR and MS. Short reaction time, easy and quick isolation of the products, and excellent yields are the main advantages of this procedure.展开更多
Severe acute respiratory syndrome coronavirus 2(SARS‐CoV‐2)continues to evolve,generating new variants that pose a threat to global health;therefore,it is imperative to obtain safe and broad‐spectrum antivirals aga...Severe acute respiratory syndrome coronavirus 2(SARS‐CoV‐2)continues to evolve,generating new variants that pose a threat to global health;therefore,it is imperative to obtain safe and broad‐spectrum antivirals against SARS‐CoV‐2 and its variants.To this end,we screened compounds for their ability to inhibit viral entry,which is a critical step in virus infection.Twenty compounds that have been previously reported to inhibit SARS‐CoV‐2 replication were tested by using pseudoviruses containing the spike protein from the original strain(SARS‐CoV‐2‐WH01).The cytotoxicity of these compounds was determined.Furthermore,we identified six compounds with strong antagonistic activity against the WH01 pseudovirus,and low cytotoxicity was identified.These compounds were then evaluated for their efficacy against pseudoviruses expressing the spike protein from B.1.617.2(Delta)and B.1.1.529(Omicron),the two most prevalent circulating strains.These assays demonstrated that two phenothiazine compounds,trifluoperazine 2HCl and thioridazine HCl,inhibit the infection of Delta and Omicron pseudoviruses.Finally,we discovered that these two compounds were highly effective against authentic SARS‐CoV‐2 viruses,including the WH01,Delta,and Omicron strains.Our study identified potential broad‐spectrum SARS‐CoV‐2 inhibitors and provided insights into the development of novel therapeutics.展开更多
基金Education Department of Zhejiang Province(No.20060811) for the financial support of this work.
文摘A simple and efficient procedure for the synthesis of substituted benzothiazoles through condensation of 2-aminothiophenol with aromatic aldehydes in the presence of H2O2/HCl system in ethanol at room temperature is described. The target compounds have been characterized by ^1H NMR, ^13C NMR, IR and MS. Short reaction time, easy and quick isolation of the products, and excellent yields are the main advantages of this procedure.
基金supported by grants from National Key R&D Program of China(2020YFA0707600 to Z.Z.and X.L.)the National Natural Science Foundation of China(81930063 and 81971948 to J.W.and X.L.)hinese Academy of Medical Science(CAMS)Innovation Fund for Medical Sciences(2021-I2M-1-038 to J.W.)。
文摘Severe acute respiratory syndrome coronavirus 2(SARS‐CoV‐2)continues to evolve,generating new variants that pose a threat to global health;therefore,it is imperative to obtain safe and broad‐spectrum antivirals against SARS‐CoV‐2 and its variants.To this end,we screened compounds for their ability to inhibit viral entry,which is a critical step in virus infection.Twenty compounds that have been previously reported to inhibit SARS‐CoV‐2 replication were tested by using pseudoviruses containing the spike protein from the original strain(SARS‐CoV‐2‐WH01).The cytotoxicity of these compounds was determined.Furthermore,we identified six compounds with strong antagonistic activity against the WH01 pseudovirus,and low cytotoxicity was identified.These compounds were then evaluated for their efficacy against pseudoviruses expressing the spike protein from B.1.617.2(Delta)and B.1.1.529(Omicron),the two most prevalent circulating strains.These assays demonstrated that two phenothiazine compounds,trifluoperazine 2HCl and thioridazine HCl,inhibit the infection of Delta and Omicron pseudoviruses.Finally,we discovered that these two compounds were highly effective against authentic SARS‐CoV‐2 viruses,including the WH01,Delta,and Omicron strains.Our study identified potential broad‐spectrum SARS‐CoV‐2 inhibitors and provided insights into the development of novel therapeutics.
