antiviral agents

Idoxuridine (Dendrid) 是一种抑制病毒 DNA 合成的脱氧尿苷类似物，用作抗病毒剂。

Tenofovir (GS 1278) 是一种核苷酸逆转录酶抑制剂，可研究 HIV 和慢性乙型肝炎。

Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) 是有机阴离子转运多肽 1B(OATP1B) 和 OATP1B3抑制剂，IC50分别为 1.5 µM 和 3.27 µM。它也具有口服活性的 HCV NS5A 蛋白抑制剂，多种 HCV 复制子基因型的 EC50范围为 9-146 pM。

Darunavir (TMC114) 是一种 HIV 蛋白酶抑制剂，用于治疗艾滋病和 HIV 感染。 由于单独使用时会出现抗病毒药物耐药性，因此与其他抗 HIV 药物联合使用。

2'-Deoxy-2'-fluorouridine 是合成抗流感病毒试剂的中间体。

2,5-PYRIDINEDICARBOXYLIC ACID 用于制备新的衍生物作为抗病毒剂。

4-(3-chlorophenyl)-2,3-dihydro-1,3-thiazol-2-one 已被用作合成多种生物活性化合物的起始材料，包括抗真菌剂、抗病毒剂和抗炎剂。

6-ethenylquinoline 是一种结构独特的芳香杂环化合物，是生产其他芳香族化合物的重要中间体，并被用作合成各种药物的起始材料，包括抗真菌剂、抗寄生虫剂和抗病毒剂。它已被证明是多种参与药物代谢的酶的抑制剂，包括细胞色素P450、醛氧化酶和黄嘌呤氧化酶等。

5-Et-ddU, Structure-activity relationships of pyrimidine nucleosides as antiviral agents for human immunodeficiency virus type 1 in peripheral blood mononuclear cells.

Darunavir Ethanolate (UIC 94017) 是一种HIV 蛋白酶抑制剂，可以用于 HIV AIDS 的相关研究。对野生型 HIV-1 蛋白酶的Ki 值为1 nM。

(E)-5-(2-Bromovinyl)uracil (BVU) is a pyrimidine base and an inactive metabolite of the antiviral agents sorivudine and (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) that may be regenerated to BVDU in vivo. BVU irreversibly inactivates dihydropyrimidine dehydrogenase (DPD) in an NADPH-dependent manner. It enhances the efficacy of the chemotherapeutic agent and DPD substrate 5-fluorouracil in a P388 murine leukemia model when administered at a dose of 200 μmol kg, increasing survival time.

Methyl 3,4-dihydroxyphenylacetate is a polyphenol that has been found inI. aquifoliumseeds and has antioxidant and antiviral activities.1,2It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50= 0.0025 mg ml).1Methyl 3,4-dihydroxyphenylacetate (0.01 μg ml) inhibits enterovirus 71 replication in rhabdomyosarcoma cells.2 1.Nahar, L., Russell, W.R., Middleton, M., et al.Antioxidant phenylacetic acid derivatives from the seeds of Ilex aquifoliumActa Pharm.55(2)187-193(2005) 2.Wang, L., Wang, J., Wang, L., et al.Anti-enterovirus 71 agents of natural productsMolecules20(9)16320-16333(2015)

4-(N-Boc-amino)piperidine is an organic building block.1,2It has been used in the synthesis of aminopiperidine antiviral chemokine (C-C motif) receptor 5 (CCR5) antagonists and antibacterial agents. 1.Burrows, J.N., Cumming, J.G., Fillery, S.M., et al.Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureasBioorg. Med. Chem. Lett.15(1)25-28(2005) 2.Reck, F., Alm, R., Brassil, P., et al.Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II: Broad-spectrum antibacterial agents with reduced hERG activityJ. Med. Chem.54(22)7834-7847(2011)

Ribavirin-13C5is intended for use as an internal standard for the quantification of ribavirin by GC- or LC-MS. Ribavirin is an antiviral guanosine nucleoside analog.1,2Upon entry into cells, ribavirin is metabolized to an active triphosphate form that induces viral RNA chain termination and inhibits viral polymerases. It reduces replication in a panel of seven RNA and four DNA viruses in Vero cells (EC50s = 2-95 μg/ml).3Ribavirin also reduces replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero cells (EC50= 109.5 μM).4Aerosol administration of ribavirin (30 mg/kg) reduces mortality in a mouse model of influenza A infection.5Formulations containing ribavirin have been used in the treatment of respiratory syncytial virus (RSV), hepatitis C virus (HCV), and viral hemorrhagic fevers. 1.Gilbert, B.E., and Knight, V.Biochemistry and clinical applications of ribavirinAntimicrob. Agents Chemother.30(2)201-205(1986) 2.Gordon, C.J., Tchesnokov, E.P., Woolner, E., et al.Remdesivir is a direct-acting antiviral that inhibits RNA-dependent RNA polymerase from severe acute respiratory syndrome coronavirus 2 with high potencyJ. Biol. Chem.295(20)6785-6797(2020) 3.Kirsi, J.J., North, J.A., McKernan, P.A., et al.Broad-spectrum antiviral activity of 2-β-D-ribofuranosylselenazole-4-carboxamide, a new antiviral agentAntimicrob. Agents Chemother.24(3)353-361(1983) 4.Wang, M., Cao, R., Zhang, L., et al.Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitroCell Res.30(3)269-271(2020) 5.Wilson, S.Z., Knight, V., Wyde, P.R., et al.Amantadine and ribavirin aerosol treatment of influenza A and B infection in miceAntimicrob. Agents Chemother.17(4)642-648(1980)

Antiviral agent 5 is a crucial intermediate utilized in the development of antiviral agents that specifically target 3C and 3CL proteases, which includes the SARS-CoV-2 M pro enzyme.

Ensitrelvir (S-217622) fumarate is a novel orally active inhibitor, targeting the SARS-CoV-2 3CL protease (IC50 = 13 nM). It demonstrates non-covalent and non-peptidic characteristics. This compound represents a pioneering advancement in the development of effective antiviral agents against the SARS-CoV-2 virus.

Deleobuvir sodium is the salt form of Deleobuvir, also known as BI207127, a non-nucleoside hepatitis C virus NS5B polymerase inhibitor for the treatment of hepatitis C. Deleobuvir was tested in combination regimens with pegylated interferon and ribavirin, and in interferon-free regimens with other direct-acting antiviral agents including faldaprevir. Deleobuvir showed that a triple combination of deleobuvir, faldaprevir, and ribavirin performed well in HCV genotype 1b patients. Efficacy fell below 50%, however, for dual regimens without ribavirin and for genotype 1a patients. In December 2013, deleobuvir was discontinued since recent findings from phase III trials did not suggest sufficient efficacy.

Thiocarbazate, also known as CID16725315, is an inhibitor of human cathepsin L. Inhibition of cathepsin L thus holds promise for therapeutic intervention for both SARS-CoV and Ebola virus infection. With respect to the development of antiviral agents, inhibitors of human cathepsin L are not subject to resistance because of rapid mutations of the viral genome. Cathepsin L is therefore an attractive target for drug development.

3'-DMTr-dG(iBu)是一种应用于核酸合成的核苷，专用于合成用于研究乙型肝炎病毒(HBV)、丁型肝炎病毒(HDV)感染治疗的抗病毒剂，以及开发针对阿尔茨海默病和其他tau蛋白病治疗的寡核苷酸。