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Total Synthesis of Tipranavir Based on Iridium-Catalyzed Asymmetric Allylic Substitution of Dihydropyranone.
Org Lett
November 2024
College of Material, Chemistry and Chemical Engineering, Hangzhou Normal University, 2318 Yuhangtang Road, Hangzhou 311121, P. R. of China.
An efficient and highly enantioselective synthesis of tipranavir is realized based on an iridium-catalyzed asymmetric allylic substitution. High yield and diastereoselectivity (>20:1), as well as excellent enantioselectivity (99% ), were obtained for the key intermediate through direct asymmetric alkylation reaction of dihydropyranone with allylic -butyl carbonate. Anti-AIDS drug of tipranavir was finally accomplished in 8 steps and 6 pots starting from commercially available 1-phenyl-3-hexanone in 20.
View Article and Find Full Text PDFPharmacokinetics of Antiretroviral Drugs in Older People Living with HIV, Part II: Drugs Licensed Before 2005.
Clin Pharmacokinet
December 2024
Sérgio Arouca National School of Public Health ENSP Fiocruz, Rio de Janeiro, RJ, Brazil.
Background And Objective: Advances in antiretroviral therapy led to an increase in life expectancy among people living with human immunodeficiency virus (HIV). As aging is characterized by several physiological changes that can influence pharmacokinetics (PK), this systematic review aims to describe the impact of aging on the PK of antiretrovirals (ARV) approved by the Food and Drug Administration (FDA) before 2005.
Methods: Searches were performed in BVS, EMBASE, and PubMed databases for publications until June 2024.
Pretreatment drug resistance among people living with HIV from 2018 to 2022 in Guangzhou, China.
J Med Virol
October 2024
Guangzhou Medical Research Institute of Infectious Diseases, Guangzhou Eighth People's Hospital, Guangzhou Medical University, Guangzhou, China.
The presence of pretreatment drug resistance (PDR) is posing an increasing threat to HIV control. Here we investigated drug resistance mutations (DRMs) and PDR among 6831 HIV-infected individuals from 2018 to 2022 in Guangzhou, China. DRMs were detected among 24.
View Article and Find Full Text PDFQuantitative Prediction of Human Immunodeficiency Virus Drug Resistance.
Viruses
July 2024
Department of Bioinformatics, Institute of Biomedical Chemistry, 10-7, Pogodinskaya Street, Moscow 119121, Russia.
Drug resistance of pathogens, including viruses, is one of the reasons for decreased efficacy of therapy. Considering the impact of HIV type 1 (HIV-1) on the development of progressive immune dysfunction and the rapid development of drug resistance, the analysis of HIV-1 resistance is of high significance. Currently, a substantial amount of data has been accumulated on HIV-1 drug resistance that can be used to build both qualitative and quantitative models of HIV-1 drug resistance.
View Article and Find Full Text PDFDengue virus: pathogenesis and potential for small molecule inhibitors.
Biosci Rep
August 2024
Regional Centre for Biotechnology, National Capital Region Biotech Science Cluster, Faridabad, India.
Dengue, caused by dengue virus (DENV), is now endemic in nearly 100 countries and infection incidence is reported in another 30 countries. Yearly an estimated 400 million cases and 2200 deaths are reported. Effective vaccines against DENV are limited and there has been significant focus on the development of effective antiviral against the disease.
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