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Assessment of the potential interactions between favipiravir and radiocontrast agents
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作者 Sonay Aydin Ozlem Celik Aydin +3 位作者 Mesut Furkan Yazar Huseyin Aydemir Mecit Kantarci Sureyya Barun 《World Journal of Radiology》 2024年第5期128-135,共8页
BACKGROUND In cases of coronavirus disease 2019(COVID-19),favipiravir is commonly included to the therapy regimen.Drug interactions between favipiravir and other COVID-19 therapy drugs are frequently researched.Howeve... BACKGROUND In cases of coronavirus disease 2019(COVID-19),favipiravir is commonly included to the therapy regimen.Drug interactions between favipiravir and other COVID-19 therapy drugs are frequently researched.However,no research on possible drug interactions between Favipiravir and radiocontrast agents,which have become almost crucial in diagnostic processes while not being part of the treatment,has been found.AIM To determine potential medication interactions between Favipiravir and radiocontrast agents.METHODS The study comprised patients who were taking Favipiravir for COVID-19 therapy and underwent a contrast-enhanced computed tomography(CT)or magnetic resonance imaging(MRI)test while taking the medicine.The computerized patient files of the cases included in the study,as well as the pharmacovigilance forms in the designated hospital,were evaluated for this purpose.RESULTS The study included the evaluation of data from 1046 patients.The study sample's mean age was 47.23±9.48 years.The mean age of cases with drug interactions was statistically significant greater than that of cases with no drug interactions(P=0.003).When evaluated with logistic regression analysis,a 1-year raises in age increases the risk of developing drug interactions by 1.63 times(P=0.023).There was no statistically significant difference in the occurrence of medication interactions between the sexes(P=0.090).Possible medication interactions were discovered in 42 cases(4%).CONCLUSION The findings of this study revealed that the most notable findings as a result of the combined use of contrast agents and favipiravir were increased creatinine and transaminase values,as well as an increase in the frequency of nausea and vomiting.The majority of drug interactions discovered were modest enough that they were not reflected in the clinic.Drug interactions become more common as people get older. 展开更多
关键词 favipiravir IOHEXOL Gadoxetic acid Meglumine gadoterate Drug interactions
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Favipiravir and its potentials in COVID-19 pandemic:An update
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作者 Dao Ngoc Hien Tam Ahmad T Qarawi +8 位作者 Mai Ngoc Luu Morgan Turnage Linh Tran Gehad Mohamed Tawfik Le Huu Nhat Minh Nguyen Tien Huy Tatsuo Iiyama Kyoshi Kita Kenji Hirayama 《Asian Pacific Journal of Tropical Medicine》 SCIE CAS 2021年第10期433-455,共23页
The COVID-19 pandemic has caused millions of deaths and hundreds of millions of confirmed infections worldwide.This pandemic has prompted researchers to produce medications or vaccines to reduce or stop the progressio... The COVID-19 pandemic has caused millions of deaths and hundreds of millions of confirmed infections worldwide.This pandemic has prompted researchers to produce medications or vaccines to reduce or stop the progression and spread of this disease.A variety of previously licensed and marketed medications are being tested for the treatment and recurrence of SARS-CoV2,including favipiravir(Avigan).Favipiravir was recognized as an influenza antiviral drug in Japan in 2014,and has been known to have a potential in vitro activity against SARS-CoV-2,in addition to its broad therapeutic safety scope.Favipiravir was recently approved and officially used in many countries worldwide.Our review provides insights and up-to-date knowledge of the current role of favipiravir in the treatment of COVID-19 infection,focusing on preclinical and ongoing clinical trials,evidence of its efficacy against SARS-CoV-2 in COVID-19,side effects,anti-viral mechanism,and the pharmacokinetic properties of the drug in the treatment of COVID-19.Due to its teratogenic effects,favipiravir cannot be offered to expectant or pregnant mothers.The practical efficacy of such an intervention regimen will depend on its dose,treatment duration,and cost as well as difficulties in application. 展开更多
关键词 favipiravir Avigan COVID-19 SARS-CoV-2 ANTIVIRAL Review EFFICACY
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Comparing the efficacy of regen-cov,remdesivir,and favipiravir in reducing invasive mechanical ventilation need in hospitalized COVID-19 patients
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作者 Sahar Kmal Hegazy Samar Tharwat Ahmed Hosny Hassan 《World Journal of Clinical Cases》 SCIE 2023年第26期6105-6121,共17页
BACKGROUND Coronavirus disease 2019(COVID-19)pandemic stimulates research works to find a solution to this crisis from starting 2020 year up to now.With ending of the 2021-year,various advances in pharmacotherapy agai... BACKGROUND Coronavirus disease 2019(COVID-19)pandemic stimulates research works to find a solution to this crisis from starting 2020 year up to now.With ending of the 2021-year,various advances in pharmacotherapy against COVID-19 have emerged.Regarding antiviral therapy,casirivimab and imdevimab antibody combination is a type of new immunotherapy against COVID-19.Standard antiviral therapy against COVID-19 includes Remdesivir and Favipiravir.AIM To evaluate the efficacy of antibodies cocktail(casirivimab and imdevimab)compared to standard antiviral therapy in reducing the need for invasive mechanical ventilation(IMV).METHODS 265 COVID-19 polymerase chain reaction confirmed patients with indication for antiviral therapy were included in this study and were divided into 3 groups(1:2:2):Group A:REGN3048-3051 antibodies cocktail(casirivimab and imdevimab),group B:Remdesivir,group C:Favipiravir.The study design is a single-blind nonrandomized controlled trial Mansoura University Hospital owns the study’s drugs.The duration of the study was about 6 mo after ethical approval.RESULTS Casirivimab and imdevimab achieve less need for O2 therapy and IMV,with less duration of this need than remdesivir and favipiravir.CONCLUSION Group A(casirivimab and imdevimab)achieve better clinical outcomes than groups B(remdesivir)and C(favipiravir)intervention groups. 展开更多
关键词 ANTIVIRALS Casirivimab and imdevimab Coronavirus disease 2019 favipiravir Remdesivir
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Favipiravir:a promising investigational agent in preventing infection and progression of COVID-19
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作者 Sidharth Mehta Himanshi Tanwar Pooja Rani 《Clinical Research Communications》 2022年第1期33-40,共8页
In late Dec.2019,a huge number of pneumonia cases caused by novel coronavirus were reported in China.2019-nCoV pandemic has influenced on millions of people's life across the world.This novel coronavirus was ident... In late Dec.2019,a huge number of pneumonia cases caused by novel coronavirus were reported in China.2019-nCoV pandemic has influenced on millions of people's life across the world.This novel coronavirus was identified to be similar with MERS and SARS.Therefore,researchers and academicians across the world still trying to find out vaccines,new drug molecules against SARS-CoV-2.The principle point of this review article is to explain the activity of favipiravir in preventing COVID-19.In view of constrained data available in the literature,we specify that favipiravir treatment,among all other anti-viral drugs,accompanied by oxygen inhalation therapy,maintaining fluid and electrolyte balance,and nutritional support may be helpful in fighting COVID-19.Researches were done on already approved existing anti-viral drugs for treating ebola virus,influenza virus infection and many such anti-viral agents like favipiravir,ritonavir,remdesivir,ribavirin,oseltamivir shows promising results in preventing COVID-19 infection and their clinical trials are currently undergoing in order to discover proper treatment of COVID-19.Among the aforementioned drug candidates,a broad-spectrum RNA polymerase inhibitor favipiravir,which demonstrated a promising tolerance profile and anti-viral efficacy in patients having COVID-19 manifestations. 展开更多
关键词 antiviral drugs clinical trial CORONAVIRUS COVID-19 favipiravir RNA polymerase inhibitor SARS-CoV-2
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Structural Basis of SARS-CoV-2 Polymerase Inhibition by Favipiravir 被引量:5
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作者 Qi Peng Ruchao Peng +5 位作者 Bin Yuan Min Wang Jingru Zhao Lifeng Fu Jianxun Qi Yi Shi 《The Innovation》 2021年第1期164-172,共9页
The outbreak of severe acute respiratory syndrome coronavirus 2(SARSCoV-2)has developed into an unprecedented global pandemic.Nucleoside analogs,such as Remdesivir and Favipiravir,can serve as the firstline broad-spec... The outbreak of severe acute respiratory syndrome coronavirus 2(SARSCoV-2)has developed into an unprecedented global pandemic.Nucleoside analogs,such as Remdesivir and Favipiravir,can serve as the firstline broad-spectrum antiviral drugs by targeting the viral polymerases.However,the underlying mechanisms for the antiviral efficacies of these drugs are far from well understood.Here,we reveal that Favipiravir,as a pyrazine derivative,could be incorporated into the viral RNA products by mimicking both adenine and guanine nucleotides.This drug thus inhibits viral replication mainly by inducing mutations in progeny RNAs,different from Remdesivir or other RNA-terminating nucleoside analogs that impair the elongation of RNA products.We further determined the cryo-EM structure of Favipiravir bound to the replicating polymerase complex of SARSCoV-2 in the pre-catalytic state.This structure provides a missing snapshot for visualizing the catalysis dynamics of coronavirus polymerase,and reveals an unexpected base-pairing pattern between Favipiravir and pyrimidine residues that may explain its capacity for mimicking both adenine and guanine nucleotides.These findings shed light on the mechanism of coronavirus polymerase catalysis and provide a rational basis for developing antiviral drugs to combat the SARS-CoV-2 pandemic. 展开更多
关键词 SARS-CoV-2 favipiravir CRYO-EM POLYMERASE pre-catalytic state
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Advanced researches on the inhibition of influenza virus by Favipiravir and Baloxavir
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作者 Qiongqiong Fang Dayan Wang 《Biosafety and Health》 2020年第2期64-70,共7页
Anti-influenza drugs are one of themost critical pathways for control of influenza virus infection.Drugs that have been developed or are developing may function via different mechanisms,and so far,inhibitors of influe... Anti-influenza drugs are one of themost critical pathways for control of influenza virus infection.Drugs that have been developed or are developing may function via different mechanisms,and so far,inhibitors of influenza virus polymerase are among the most promising types of drugs.Favipiravir and Baloxavir,also named T-705 and Xofluza respectively,have been approved for influenza treatment in Japan and the United States.Favipiravir effectively and selectively inhibits the RNA-dependent RNA polymerase(RdRp)of RNA viruses while Baloxavir specifically targets the cap-dependent endonuclease PA of influenza viruses.These two drugs have been suggested as the first candidate drugs for influenza infection treatment,especially for strains resistant to other anti-influenza drugs.This review will focus on the pharmaceutical mechanisms and anti-influenza activity of these two drugs. 展开更多
关键词 favipiravir Baloxavir Influenza virus Anti-influenza drug Drug target
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法匹拉韦的合成 被引量:13
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作者 王皖 刘敏 +1 位作者 肖新荣 戴秋云 《国际药学研究杂志》 CAS CSCD 北大核心 2015年第2期220-224,共5页
目的设计并探索一条工艺稳定、收率较高的抗病毒化合物法匹拉韦(T-705)的合成工艺路线。方法以氨基丙二酸二乙酯盐酸盐为起始原料,氨水氨解后与乙二醛环合得到3-羟基-2-吡嗪酰胺、经硝酸钾硝化后制得3-羟基-6-硝基-2-吡嗪酰胺,再经三氯... 目的设计并探索一条工艺稳定、收率较高的抗病毒化合物法匹拉韦(T-705)的合成工艺路线。方法以氨基丙二酸二乙酯盐酸盐为起始原料,氨水氨解后与乙二醛环合得到3-羟基-2-吡嗪酰胺、经硝酸钾硝化后制得3-羟基-6-硝基-2-吡嗪酰胺,再经三氯氧磷氯代、氟化钾氟代制得3,6-二氟-2-氰基吡嗪,水解成盐,最后经过氧化氢(双氧水)氧化制得目标化合物法匹拉韦。结果设计出的合成路线能有效制备目标化合物。结论该合成路线各步反应中除氟取代需要严格去水外,其余各步反应条件较温和且操作简单、收率稳定,适合规模制备。 展开更多
关键词 抗病毒化合物 法匹拉韦 合成
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法匹拉韦用于病毒感染性疾病的国内外文献分析 被引量:3
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作者 苏娜 刘颖 +2 位作者 陈小艺 魏春燕 何治尧 《医药导报》 CAS 北大核心 2020年第7期930-935,共6页
目的检索法匹拉韦用于病毒感染性疾病的研究,评价法匹拉韦的有效性和安全性,为法匹拉韦治疗新型冠状病毒肺炎(COVID-19)提供参考。方法检索Ovid EMBase、Ovid Medline、Ovid CENTRAL和中国知网(CNKI)等数据库,纳入法匹拉韦用于病毒感染... 目的检索法匹拉韦用于病毒感染性疾病的研究,评价法匹拉韦的有效性和安全性,为法匹拉韦治疗新型冠状病毒肺炎(COVID-19)提供参考。方法检索Ovid EMBase、Ovid Medline、Ovid CENTRAL和中国知网(CNKI)等数据库,纳入法匹拉韦用于病毒感染性疾病的临床研究,并进行描述性分析。结果初检文献265篇,覆盖23种病毒,筛选后纳入11篇法匹拉韦治疗病毒感染性疾病的临床研究,涉及5种病毒性疾病:流行性感冒(流感)4篇,埃博拉(EBO)出血热3篇,严重发热和血小板减少综合征(SFTS)1篇,拉沙(LAS)出血热1篇,新型冠状病毒肺炎(COVID-19)1篇,安全性相关研究1篇。研究结果显示,法匹拉韦用于流感、EBO、SFTS、LAS、COVID-19临床疗效较好,其中用于COVID-19的研究结果显示法匹拉韦治疗组病毒转阴时间中位数4 d(IQR:2.5~9),明显小于对照组的11 d(IQR:8~13)(P<0.001)。结论法匹拉韦临床研究的报道较少,动物和细胞研究较多,临床研究显示其有良好疗效,可推荐用于治疗COVID-19。 展开更多
关键词 法匹拉韦 新型冠状病毒肺炎 病毒感染性疾病
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基于分子对接技术精细分析中药化学成分与新型冠状病毒RNA聚合酶之间的结合模式 被引量:7
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作者 彭安堂 苏彦雷 +6 位作者 刘倩 常希龙 汪俊松 霍长虹 王建荣 段绪红 师洋 《中华中医药学刊》 CAS 北大核心 2021年第4期94-101,I0034-I0039,共14页
以SARS RNA聚合酶6NUR为模板,采用同源建模方法,构建出了新型冠状病毒RNA聚合酶的三维结构模型,以之为抗病毒的研究靶点,精细分析靶酶中NTPs结合位点处氨基酸与底物抑制剂的分子间相互作用,虚拟筛选得出黄酮类化合物为抗新型冠状病毒活... 以SARS RNA聚合酶6NUR为模板,采用同源建模方法,构建出了新型冠状病毒RNA聚合酶的三维结构模型,以之为抗病毒的研究靶点,精细分析靶酶中NTPs结合位点处氨基酸与底物抑制剂的分子间相互作用,虚拟筛选得出黄酮类化合物为抗新型冠状病毒活性较强成分,研究结果被证明与抗疫临床治疗实践具有非常高的关联性,亦与某些黄酮类化合物为NS5B抑制剂从而具有抗丙型肝炎病毒活性的现实相符合,故认为以黄酮类化合物为代表的某些中药成分是抗新型冠状病毒的有效成分,希望能引起国内外科研人员的注意,能进一步的实验验证,助力于早日研发成功更好的抗新型冠状病毒药物。 展开更多
关键词 新型冠状病毒 中医 RNA聚合酶 同源建模 6NUR 6M71 分子对接 抑制剂 瑞德西韦 法匹拉韦 黄酮 丙型肝炎病毒 NS5B
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抗新型冠状病毒候选药物法维拉韦首批国家对照品的研制 被引量:3
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作者 熊婧 严菁 +2 位作者 刘毅 刘阳 何兰 《中国药物警戒》 2022年第1期52-56,61,共6页
目的为有效控制法维拉韦片的产品质量,满足企业注册上市及生产的需要,研制法维拉韦首批含量测定用于国家化学对照品。方法采用质谱、核磁共振谱和红外光谱进行结构确证,利用高效液相色谱法进行有关物质分析及均匀性、稳定性考察,采用气... 目的为有效控制法维拉韦片的产品质量,满足企业注册上市及生产的需要,研制法维拉韦首批含量测定用于国家化学对照品。方法采用质谱、核磁共振谱和红外光谱进行结构确证,利用高效液相色谱法进行有关物质分析及均匀性、稳定性考察,采用气相色谱法、水分测定法、动态蒸气吸附法和炽灼残渣检查法对其他理化性质进行检查,采用质量平衡法进行含量赋值,并通过氟核磁共振定量法、进口对照品外标法以及差示扫描量热法对含量结果的准确性进行验证。结果确证了法维拉韦首批国家对照品的结构,并确定其含量为99.7%。结论法维拉韦首批国家对照品具备纯度高、量值准确、稳定性好的特性,可有效控制产品质量。 展开更多
关键词 法维拉韦 新型冠状病毒肺炎 对照品 标准物质 质量平衡法 核磁共振定量 动态蒸气吸附法
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Convalescent plasma therapy in a pregnant COVID-19 patient with a dramatic clinical and imaging response: A case report
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作者 Ramezan Jafari Nematollah Jonaidi-Jafari +1 位作者 Fatemeh Dehghanpoor Amin Saburi 《World Journal of Radiology》 CAS 2020年第7期137-141,共5页
BACKGROUND Coronavirus disease 2019(COVID-19)is a novel very contagious infection which was designated a pandemic in all countries of the world in April 2020.Its presentation varies from mild to severe infection,but t... BACKGROUND Coronavirus disease 2019(COVID-19)is a novel very contagious infection which was designated a pandemic in all countries of the world in April 2020.Its presentation varies from mild to severe infection,but the majority of infected patients have mild manifestations.Many therapeutic choices have been suggested to treat the infection,but none are fully effective.CASE SUMMARY Herein we present a 26-year-old woman with a twin pregnancy at 36 wk and one day gestation with confirmed COVID-19 who responded dramatically to convalescent plasma therapy(CPT)and Favipiravir.CONCLUSION Although this case report shows the efficacy of CPT in addition to usual medications used for COVID-19,there are many questions that need to be answered regarding dosage,para-clinical efficacy,side effects and combination therapy. 展开更多
关键词 Case report Convalescent plasma therapy Pregnancy COVID-19 favipiravir Radiologic findings
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以RNA依赖的RNA聚合酶为靶点的抗新型冠状病毒抑制剂筛选 被引量:14
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作者 苏彦雷 段绪红 +2 位作者 许文成 赵玲 关世奎 《中华中医药学刊》 CAS 北大核心 2020年第5期7-13,I0011,I0012,共9页
目的从理论上筛选出新型冠状病毒(SARS-CoV-2)的RNA依赖的RNA聚合酶(RdRp)抑制剂。方法依据SARS-CoV-2的RNA聚合酶与SARS聚合酶结构(6NUR)具有高度的同源性,以SARS的RNA聚合酶为模板构建SARS-CoV-2的RNA聚合酶的三维结构,利用分子对接软... 目的从理论上筛选出新型冠状病毒(SARS-CoV-2)的RNA依赖的RNA聚合酶(RdRp)抑制剂。方法依据SARS-CoV-2的RNA聚合酶与SARS聚合酶结构(6NUR)具有高度的同源性,以SARS的RNA聚合酶为模板构建SARS-CoV-2的RNA聚合酶的三维结构,利用分子对接软件Autodock Vina研究选中15个化合物与模型靶酶的相互作用,评估化合物对SARS-CoV-2的RNA聚合酶的抑制活性。结果研究发现,所选化合物均与靶酶的活性位点有一定相互作用,其中瑞德西韦活性形式、法匹拉韦活性形式、黄酮及异黄酮类化合物与靶酶的相互作用较强,以瑞德西韦活性形式与靶酶的结合能最低(为-7.9kal/mol),化合物1、2、8、13、14与酶的结合作用相对弱,提示对靶酶的抑制活性弱于瑞德西韦等,而化合物15没有酶抑制活性。结论通过虚拟筛选,得到了SARS-CoV-2 RNA聚合酶的一些抑制剂,其中的某些中药"活性成分"与目前临床上应用方剂的疗效具有较大的相关性,与清肺排毒汤等中医药治疗方案相互佐证。本研究为开发实施有效的抗新型冠状病毒治疗方案提供一定的理论参考,具体作用机制可进行进一步深入的研究验证。 展开更多
关键词 新型冠状病毒 RNA聚合酶 抑制剂 筛选 分子对接 瑞德西韦 法拉匹韦 黄酮
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法匹拉韦治疗新型冠状病毒肺炎的可行性分析 被引量:6
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作者 张竞文 胡欣 金鹏飞 《中国药业》 CAS 2020年第6期20-24,共5页
目的 探讨法匹拉韦治疗新型冠状病毒肺炎(COVID-19)的临床可行性。方法 针对从已上市/已进入临床研究的药物中挖掘出的、可能具有抗新型冠状病毒(SARS-CoV-2)作用的药物之一法匹拉韦,结合其作用机制、临床应用史和临床疗效及安全性试验... 目的 探讨法匹拉韦治疗新型冠状病毒肺炎(COVID-19)的临床可行性。方法 针对从已上市/已进入临床研究的药物中挖掘出的、可能具有抗新型冠状病毒(SARS-CoV-2)作用的药物之一法匹拉韦,结合其作用机制、临床应用史和临床疗效及安全性试验进行可行性分析。结果 与结论法匹拉韦为国内首个在疫情期间批准上市的抗病毒药物,适应证为成人新型或再次流行的流感。经可行性分析,其对多种RNA病毒疗效显著,且不良反应也较少,从理论上对SARS-CoV-2也有作用,但有待更大规模的临床试验进行验证。 展开更多
关键词 新型冠状病毒 严重急性呼吸综合征 新型冠状病毒肺炎 法匹拉韦 可行性
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基于静电势电荷的抗击埃博拉病毒新药物法匹拉韦及其衍生物水溶解度logS值预测 被引量:2
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作者 裴诗恩 黄颖琦 +5 位作者 吴淑曼 彭自珍 苏凌峰 刘喜灵 陈晗剑 钟爱国 《当代化工》 CAS 2017年第1期31-34,共4页
运用分子中的原子理论(AIM),探讨了以法匹拉韦分子羰基氧原子值为目标,测试了不同基组和泛函选择的依赖性。然后用密度泛函理论(DFT B3LYP)和6-31+G(d,p)基组,优化了20种法匹拉韦及其常见衍生物的分子结构,分别得到11号羰基氧的密立根电... 运用分子中的原子理论(AIM),探讨了以法匹拉韦分子羰基氧原子值为目标,测试了不同基组和泛函选择的依赖性。然后用密度泛函理论(DFT B3LYP)和6-31+G(d,p)基组,优化了20种法匹拉韦及其常见衍生物的分子结构,分别得到11号羰基氧的密立根电荷(MUL-O)、自然原子轨道电荷(NBO-O)、何秀巴赫电荷(HIR-O)和静电势电荷(ESP-O)值,发现11号氧原子的ESP-O电荷值与用ACD Lab6.0预测出来的log S值相关性最好,相关系数达0.986;计算了法匹拉韦及其11种未知衍生物的ESP-O电荷值,代入相关最佳线性方程,发现所得结果与ACD Lab6.0预测结果十分接近,最大误差绝对对数值仅为0.08;分子的静电势图也显示法匹拉韦及其甲基法匹拉韦发挥其药理毒理作用可能的部位在电负性强的羰基氧原子上。 展开更多
关键词 密度泛函理论 法匹拉韦 Mulliken电荷 NBO电荷 ESP电荷 LOG S值
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抗埃博拉病毒药物法匹拉韦及其衍生物pK_b值预测 被引量:2
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作者 李余 裴诗恩 +5 位作者 乔骏驰 彭自珍 苏凌峰 刘喜灵 陈晗剑 钟爱国 《当代化工》 CAS 2016年第7期1503-1505,共3页
运用密度泛函理论(DFT B3LYP)和6-31+G(d,p)基组,优化了20种法匹拉韦衍生物的分子结构,分别得到羰基氧的Mulliken、NBO和ESP电荷值,发现其Mulliken电荷值与用ACD Lab6.0预测出来的p Kb值相关性最好,相关系数达0.976;计算了法匹拉韦及其1... 运用密度泛函理论(DFT B3LYP)和6-31+G(d,p)基组,优化了20种法匹拉韦衍生物的分子结构,分别得到羰基氧的Mulliken、NBO和ESP电荷值,发现其Mulliken电荷值与用ACD Lab6.0预测出来的p Kb值相关性最好,相关系数达0.976;计算了法匹拉韦及其11种衍生物的Mulliken电荷值,带入相关线性方程,发现所得结果与ACD Lab6.0预测结果十分接近,最大误差绝对值仅为0.08,由此也得知法匹拉韦发挥其药理毒理作用可能的部位在羰基氧上。 展开更多
关键词 密度泛函理论 法匹拉韦 Mulliken电荷 NBO电荷 pKb值
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法匹拉韦的合成 被引量:6
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作者 任昱霖 刘丰良 《广州化工》 CAS 2017年第18期52-53,共2页
以3-氨基-2-羧基吡嗪为原料,经酯化反应、溴代反应生成化合物3,再经重氮化反应、氨解反应、氯代反应生成6,最后经苯环氟代反应、氰基水解反应、羟基取代反应即一锅煮反应合成法匹拉韦,总收率为26%。本文对酯化反应、溴代反应、氨解反应... 以3-氨基-2-羧基吡嗪为原料,经酯化反应、溴代反应生成化合物3,再经重氮化反应、氨解反应、氯代反应生成6,最后经苯环氟代反应、氰基水解反应、羟基取代反应即一锅煮反应合成法匹拉韦,总收率为26%。本文对酯化反应、溴代反应、氨解反应等反应过程中的反应条件等进行了优化;同时,其关键中间体3、6采用重结晶法纯化;最后3步反应采用一锅法完成,简化了操作。 展开更多
关键词 3-氨基-2-羧酸吡嗪 合成 法匹拉韦
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法匹拉韦抗新型冠状病毒的机制研究进 展 被引量:1
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作者 阿热依·巴哈提 王均琪 +6 位作者 祝娜 白颖璐 曹靖宜 张明烁 张严 李志勇 黄秀兰 《医药导报》 CAS 北大核心 2022年第11期1651-1659,共9页
新型冠状病毒肺炎(COVID-19)是一种由严重急性呼吸综合征冠状病毒2型(SARS-CoV-2)所致的传染病,自2019年末以来在全球迅速传播。当前科学界正进行前所未有的努力,研究该病毒感染的潜在机制并提出合理的临床应用药物,以降低COVID-19发病... 新型冠状病毒肺炎(COVID-19)是一种由严重急性呼吸综合征冠状病毒2型(SARS-CoV-2)所致的传染病,自2019年末以来在全球迅速传播。当前科学界正进行前所未有的努力,研究该病毒感染的潜在机制并提出合理的临床应用药物,以降低COVID-19发病率。法匹拉韦(favipiravir)是一种RNA依赖性RNA聚合酶(RdRp)抑制剂,在中国被批准用于治疗COVID-19。该文概述法匹拉韦通过结合SARS-CoV-23种关键病毒酶RdRp、3-胰凝乳蛋白酶样半胱氨酸蛋白酶(3CLpro)和木瓜蛋白酶样蛋白酶(PLpro)抑制SARS-CoV-2的机制,并综述法匹拉韦与上述病毒蛋白酶的分子对接数据。 展开更多
关键词 法匹拉韦 新型冠状病毒肺炎 RNA依赖性RNA聚合酶 3-胰凝乳蛋白酶样半胱氨酸蛋白酶 木瓜蛋白酶样蛋白酶
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从专利的角度看抗病毒药物法匹拉韦的研究进展 被引量:4
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作者 张珮明 刘琳 雷耀龙 《中国发明与专利》 2020年第5期50-57,共8页
法匹拉韦是一种广谱抗RNA病毒药物。本文概述了法匹拉韦的发展历程及专利态势,并在检索、整理、分析和归纳相关专利的基础上,主要围绕法匹拉韦结构改进、制剂设计、制备工艺优化以及药物新用途等方面进一步阐述了法匹拉韦专利技术发展情... 法匹拉韦是一种广谱抗RNA病毒药物。本文概述了法匹拉韦的发展历程及专利态势,并在检索、整理、分析和归纳相关专利的基础上,主要围绕法匹拉韦结构改进、制剂设计、制备工艺优化以及药物新用途等方面进一步阐述了法匹拉韦专利技术发展情况,为其后续的研发与临床应用提供参考依据。 展开更多
关键词 法匹拉韦 制剂 药物联用 RNA聚合酶 抗病毒
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顶空气相色谱法同时测定法匹拉韦原料药中5种有机溶剂的残留量 被引量:8
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作者 刘葵葵 邓玉晓 +1 位作者 邢学敏 王伶 《中国药房》 CAS 北大核心 2017年第24期3415-3418,共4页
目的:建立同时测定法匹拉韦原料药中乙醇、丙酮、乙酸乙酯、N,N-二异丙基乙胺、甲苯5种有机溶剂残留量的方法。方法:采用顶空气相色谱法。色谱柱为DB-624毛细管柱,程序升温,进样口温度为220℃,检测器为氢火焰离子化检测器,检测器温度为... 目的:建立同时测定法匹拉韦原料药中乙醇、丙酮、乙酸乙酯、N,N-二异丙基乙胺、甲苯5种有机溶剂残留量的方法。方法:采用顶空气相色谱法。色谱柱为DB-624毛细管柱,程序升温,进样口温度为220℃,检测器为氢火焰离子化检测器,检测器温度为250℃,载气为氮气,载气流速为2.0 mL/min,分流比为10∶1,顶空平衡温度为80℃,平衡时间为20 min,顶空进样量为1mL。结果:乙醇、丙酮、乙酸乙酯、N,N-二异丙基乙胺和甲苯检测质量浓度线性范围分别为10.0~501.4μg/mL(r=0.999 9)、10.0~501.4μg/mL(r=0.999 9)、10.1~502.6μg/mL(r=0.999 9)、0.2~11.4μg/mL(r=0.999 9)、1.8~89.4μg/mL(r=0.999 7);定量限分别为5.3、3.4、5.2、6.1、20.4μg/mL,检测限分别为1.4、1.1、1.3、1.6、5.9μg/mL;精密度试验的RSD<4.0%,稳定性、重复性试验中只检出丙酮,其RSD<4.0%;加样回收率分别为96.61%~99.70%(RSD=1.01%,n=9)、95.81%~99.50%(RSD=1.29%,n=9)、96.42%~99.76%(RSD=1.24%,n=9)、96.36%~99.30%(RSD=1.19%,n=9)、97.00%~99.51%(RSD=0.82%,n=9)。结论:该方法简单、准确、重复性好,可用于法匹拉韦原料药中5种有机溶剂残留量的同时测定。 展开更多
关键词 气相色谱法 法匹拉韦 有机溶剂 残留量 乙醇 丙酮 乙酸乙酯 N N-二异丙基乙胺 甲苯
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3种口服抗流感病毒药物药理特性及临床应用对比 被引量:4
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作者 袁世加 《中国药业》 CAS 2021年第13期123-126,共4页
目的探讨阿比多尔、奥司他韦、法匹拉韦3种口服抗流感病毒药物的药理特性,为临床的合理使用提供参考。方法通过阅读文献、药品说明书、诊疗指南等,3种口服抗流感病毒药物的药理差异。结果奥司他韦耐药性稍差,但安全性数据更完善;3种口... 目的探讨阿比多尔、奥司他韦、法匹拉韦3种口服抗流感病毒药物的药理特性,为临床的合理使用提供参考。方法通过阅读文献、药品说明书、诊疗指南等,3种口服抗流感病毒药物的药理差异。结果奥司他韦耐药性稍差,但安全性数据更完善;3种口服抗流感病毒药物的有效性无明显差异。结论3种口服抗流感病毒药物均能有效用于甲、乙型流感病毒的治疗。 展开更多
关键词 抗流感病毒药物 阿比多尔 奥司他韦 法匹那韦 有效性 安全性 耐药性
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