hcov-229e-in-1

HCoV-229E-IN-1 is a potent inhibitor of HCoV-229E replication, with an EC50 of 0.65 μM and 0.6 μM in MTS and CPE cells, respectively[1]. HCoV-229E-IN-1 (compound 5h) (0.01-100 μM) fully suppresses the capacity of HCoV-229E replication in a dose-dependent manner[1].HCoV-229E-IN-1 (12 μM) fully prevented the formation of dsRNA intermediates of CoV RNA synthesis[1]. [1]. Stevaert A, et, al. Betulonic Acid Derivatives Interfering with Human Coronavirus 229E Replication via the nsp15 Endoribonuclease. J Med Chem. 2021 May 13;64(9):5632-5644.

HRSV hCoV-229E-IN-1 (compound 8X) 是强效的HRSV和hCoV-229E抑制剂，其对hCoV-229E的IC50为2.1 µM。HRSV hCoV-229E-IN-1 能够抑制细胞活力。

HNC-1664 是一种可口服的 RNA 依赖性 RNA 聚合酶 (RdRP) 抑制剂，具有广谱抗病毒活性，针对冠状病毒 (SARS-CoV-2 野生型及其突变体 XBB.1.18、HK.3.1、BF.7.14、BA.1、HCoV-229E、HCoV-OC43) 和沙粒病毒 (arenavirus)。此外，HNC-1664 在 SARS-CoV-2 Delta 感染的小鼠模型中显示出抗感染活性。

Mpro inhibitor N3 hemihydrate is a potent inhibitor of SARS-CoV-2 Mpro with an EC50 of 16.77 μM for SARS-CoV-2. Mpro inhibitor N3 hemihydrate specifically inhibits Mpro from multiple coronaviruses, including SARS-CoV and MERS-CoV. Mpro inhibitor N3 hemihydrate displays inhibition against HCoV-229E, FIPV, and MHV-A59 with individual IC50 of 4.0 μM, 8.8 μM, and 2.7 μM, respectively[1][2]. Mpro inhibitor N3 hemihydrate (0-0.64 μM) is able to penetrate cells to inhibit the replication of IBV viruses, probably at the beginning of infection in embryos[3]. [1]. Jin Z, et al. Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors. Nature. 2020;582(7811):289-293.[2]. Yang H, et al. Design of wide-spectrum inhibitors targeting coronavirus main proteases [published correction appears in PLoS Biol. 2005 Nov;3(11):e428]. PLoS Biol. 2005;3(10):e324.[3]. Wang F, et al. Structure of Main Protease from Human Coronavirus NL63: Insights for Wide Spectrum Anti-Coronavirus Drug Design. Sci Rep. 2016;6:22677. Published 2016 Mar 7.

ARS-CoV-2-IN-53（Compd 5d）对SARS-CoV-2复制具有抑制作用，其EC50值为14.3 μM。此化合物对人类冠状病毒229E（HCoV-229E）也表现出显著的抗病毒活性。

BPR3P0128是一种口服活性非核苷类RNA依赖性RNA聚合酶 (RdRp) 抑制剂，可抑制各种SARS-CoV-2变异体活性，对SARS-CoV-2和HCoV-229E的EC50分别为0.62和0.14 µM，在亚微摩尔范围内具有高效抗泛冠状病毒活性，并与Remdesivir联用表现出协同抗病毒活性。

SARS-CoV-IN-5 (compound 49) 作为一种高选择性的非肽类非共价3CLpro抑制剂,对SARS-CoV-1、SARS-CoV-2和蝙蝠冠状病毒WIV1的3CLpro具有强效抑制作用,IC50值分别为38 nM、21.1 nM和86 nM.此外,SARS-CoV-IN-5能有效抑制SARS-CoV-2 delta变体的复制,其EC50为0.272 μM,并在K18-hACE2转基因小鼠模型中显著降低肺部病毒拷贝数.该化合物对SARS-CoV-1、WIV1、MERS、HCoV-OC43、HCoV-229E和HKU9等多种冠状病毒具有良好的抗病毒活性,显示出其广谱的潜在疗效.