Bioisosteric replacement of the carboxylic acid group in Hepatitis-C virus NS5B thumb site II inhibitors: phenylalanine derivatives.

Hepatitis C virus (HCV) is a global health concern and the NS5B RNA-dependent RNA polymerase (RdRp) of HCV is an attractive target for drug discovery due to its role in viral replication. This study focuses on NS5B thumb site II inhibitors, specifically phenylalanine derivatives, and explores bioisosteric replacement and prodrug strategies to overcome limitations associated with carboxylic acid functionality. The synthesized compounds demonstrated antiviral activity, with compound 6d showing the most potent activity with an EC value of 3.

Bioisosterism: 1,2,4-Oxadiazole Rings.

Although studies in drug discovery have gained momentum in recent years, the conversion of drugs in use today into less toxic derivatives with pharmacologically superior properties is still of great importance in drug research. Bioisosterism facilitates the conversion of drugs into derivatives that present more positive pharmacological and toxicological profiles by changing existing groups in the drug structure within the framework of certain criteria that have been expanded today. The 1,2,4-oxadiazole ring is used as a bioisostere for ester and amide groups due to its resistance to hydrolysis.

In-Situ XPS Monitoring and Characterization of Electrochemically Prepared Au Nanoparticles in an Ionic Liquid.

Gold nanoparticles (Au NPs) have been electrochemically prepared in situ and in vacuo using two different electrochemical device configurations, containing an ionic liquid (IL), --diethyl--methyl--(2-methoxyethyl)ammonium bis(trifluoromethanesulfonyl)imide, that serves both as reaction and as stabilizing media for the NPs. It was observed in both devices that Au NPs were created using an anodically triggered route. The created Au NPs are relatively small (3-7 nm) and reside within the IL medium.