In the development of central nervous system (CNS) drugs, the blood–brain barrier (BBB)
restricts many drugs from entering the brain to exert therapeutic effects. Although many …

Small molecule drugs that covalently bind irreversibly to their target proteins have several
advantages over conventional reversible inhibitors. They include increased duration of …

In the field of drug discovery, the nitrile group is well represented among drugs and
biologically active compounds. It can form both non-covalent and covalent interactions with …

Toxoplasma gondii severely threaten the health of immunocompromised patients and
pregnant women as this parasite can cause several disease, including brain and eye …

Introduction With the increasing incidence and prevalence of neurological disorders
globally, there is a paramount need for new pharmacotherapies. BBB effectively protects the …

Peptidomimetics of the class of dipeptidyl nitrile analog peptoids were synthesized as
inhibitors of mammalian cysteine proteases of the papain superfamily. The dipeptidyl nitrile …

No new drugs for treatment of toxoplasmosis have been approved in over 60 years, despite
the burden of toxoplasmosis on human society. The small selection of effective drugs is …

In this paper, we report the design, synthesis and biological investigation of a series of
peptidyl vinyl ketones obtained by modifying the P2 fragment of previously reported highly …

Emerging RNA viruses, including SARS-CoV-2, continue to be a major threat. Cell entry of
SARS-CoV-2 particles via the endosomal pathway involves cysteine cathepsins. Due to …

An efficient preparative-scale synthetic procedure of l-phenylalanine derivatives has been
developed using mutant variants of phenylalanine ammonia-lyase from Arabidopsis thaliana …