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Synthesis and structure-activity relationship study of new biaryl amide derivatives and their inhibitory effects against hepatitis C virus.
Eur J Med Chem
January 2022
Institute of Medicinal Biotechnology, Chinese Academy of Medical Science and Peking Union Medical College, Beijing, 100050, PR China. Electronic address:
A series of novel biaryl amide derivatives were synthesized and evaluated for anti-HCV virus activity. Some significant SARs were uncovered. The intensive structural modifications led to fifteen novel compounds with more potent inhibitory activity compared to the hit compounds IMB 26 and IMB1f.
View Article and Find Full Text PDFSARS-CoV-2 M inhibitors with antiviral activity in a transgenic mouse model.
Science
March 2021
State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, Sichuan 610041, China.
The COVID-19 pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) continually poses serious threats to global public health. The main protease (M) of SARS-CoV-2 plays a central role in viral replication. We designed and synthesized 32 new bicycloproline-containing M inhibitors derived from either boceprevir or telaprevir, both of which are approved antivirals.
View Article and Find Full Text PDFA computational drug repurposing approach in identifying the cephalosporin antibiotic and anti-hepatitis C drug derivatives for COVID-19 treatment.
Comput Biol Med
March 2021
Division of Life Science, Department of Bio & Medical Big Data (BK21 Four Program), Plant Molecular Biology and Biotechnology Research Center (PMBBRC), Research Institute of Natural Science (RINS), Gyeongsang National University (GNU), 501 Jinju-daero, Jinju, 52828, Republic of Korea. Electronic address:
The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has caused over 1.4 million deaths worldwide. Repurposing existing drugs offers the fastest opportunity to identify new indications for existing drugs as a stable solution against coronavirus disease 2019 (COVID-19).
View Article and Find Full Text PDFProposal of a Parameter for OATP1B1 Inhibition Screening at the Early Drug Discovery Stage.
J Pharm Sci
December 2019
Drug Metabolism and Pharmacokinetics Research Laboratory, Japan Tobacco Inc., Takatsuki 569-1125, Japan.
Article Synopsis
- The study highlights the risks associated with potent inhibitors of the OATP1B1 transporter, which can significantly elevate statin levels and lead to harmful effects.
- Researchers propose using the parameter "fu/IC" to evaluate potential drug interactions early in drug development, allowing for the elimination of compounds that might cause adverse reactions with statins.
- The analysis demonstrated that statins' exposure (measured by AUC) increased more than four times with certain inhibitors, suggesting that compounds with a fu/IC ratio greater than 0.1 L/μmol are likely to pose a high risk for interactions with statins.
Mechanistic Evaluation of the Complex Drug-Drug Interactions of Maraviroc: Contribution of Cytochrome P450 3A, P-Glycoprotein and Organic Anion Transporting Polypeptide 1B1.
Drug Metab Dispos
May 2019
Pharmacokinetics, Pharmacodynamics and Metabolism, Medicine Design, Pfizer Inc., Groton, Connecticut (E.K., R.J.S., H.E., A.D.R., M.V.S.V.); and Clinical Pharmacology, Pfizer Inc., New York, New York (M.V.).
The aim of the present study was to quantitatively evaluate the drug-drug interactions (DDIs) of maraviroc (MVC) with various perpetrator drugs, including telaprevir (TVR), using an in vitro data-informed physiologically based pharmacokinetic (PBPK) model. MVC showed significant active uptake and biliary excretion in sandwich-cultured human hepatocytes, and biphasic organic anion transporting polypeptide (OATP)1B1-mediated uptake kinetics in transfected cells (high-affinity ∼5 M). No measureable active uptake was noted in OATP1B3- and OATP2B1-transfceted cells.
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