China 
Africa 
Explore chapters and articles related to this topic
Hydrolytic Enzymes for the Synthesis of Pharmaceuticals
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Sergio González-Granda, Vicente Gotor-Fernández
Telaprevir is a serine protease inhibitor approved for the treatment of hepatitis C patients. The desymmetrisation of a meso-diol precursor using vinyl acetate as both acyl donor and solvent, and the has been efficiently catalysed by Amano PS lipase supported on Celite (Scheme 9.36), obtaining the (1S,2R)-monoacetate in 97% yield and 97% ee after 17 h at 0°C (Moni et al., 2015). In a complementary approach, its enantiomer (1R,2S)-monoacetate was obtained by chemical acetylation of the diol and subsequent desymmetrisation using the same enzyme in hydrolytic conditions, leading to the hydroxy acetate in 78% yield and 95% ee after 21 h at 20°C. Desymmetrisation of meso-compounds by independent acetylation or hydrolysis using Amano PS towards the formation of Telaprevir.
Pharmacoinformatics-based strategy in designing and profiling of some Pyrazole analogues as novel hepatitis C virus inhibitors with pharmacokinetic analysis
Published in Egyptian Journal of Basic and Applied Sciences, 2023
Stephen Ejeh, Adamu Uzairu, Gideon A. Shallangwa, Stephen E. Abechi, Muhammad Tukur Ibrahim
Infection with the Hepatitis C virus (HCV) is a major health challenge concerned with the progress of a chronic liver disease impacting up to 3% of the populace and killing over 300,000 people annually [1]. Around 1% of the globe’s population is chronically infected with HCV, putting them in potential danger of developing liver cirrhosis and hepatocellular carcinoma [2]. Developing nations (where HCV infection is prevalent) face high treatment costs. In Africa, particularly in Egypt, where HCV infection threatens a large proportion of the population, HCV treatment became one of the top national priorities from 2007 to date [3,4]. There are an estimated 2.5 to 4 million new infections per year, which indicates that the disease is becoming more widespread [5,6]. For more than a decade, the recommended treatment for HCV infection has been pegylated interferon-alpha and ribavirin. Some directly acting antivirals (DAA) have later been implemented as an aspect of combination therapies for HCV infection, including telaprevir, boceprevir, simeprevir, and sofosbuvir [7]. Despite remarkable advances in HCV therapy, the fight against these infections is far from over, owing to higher pharmacoeconomic factors as well as the emergence of mutant strains resistant to DAA drugs [8]. As a result, the search for unique, friendlier, and more potent drugs, as well as unique antiviral receptors, is ongoing [9].