Strategies for structural modification of small molecules to improve blood–brain barrier penetration: a recent perspective

B Xiong, Y Wang, Y Chen, S Xing, Q Liao… - Journal of Medicinal …, 2021 - ACS Publications
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 …

An update on the discovery and development of reversible covalent inhibitors

Faridoon, R Ng, G Zhang, JJ Li - Medicinal Chemistry Research, 2023 - Springer
Small molecule drugs that covalently bind irreversibly to their target proteins have several
advantages over conventional reversible inhibitors. They include increased duration of …

Covalent reversible inhibitors of cysteine proteases containing the nitrile warhead: recent advancement in the field of viral and parasitic diseases

S Brogi, R Ibba, S Rossi, S Butini, V Calderone… - Molecules, 2022 - mdpi.com
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 …

Impact of the recognition part of dipeptidyl nitroalkene compounds on the inhibition mechanism of cysteine proteases cruzain and cathepsin L

K Arafet, S Royo, T Schirmeister, F Barthels… - ACS …, 2023 - ACS Publications
Cysteine proteases (CPs) are an important class of enzymes, many of which are responsible
for several human diseases. For instance, cruzain of protozoan parasite Trypanosoma cruzi …

Designing drugs optimized for both blood–brain barrier permeation and intra-cerebral partition

M Dichiara, G Cosentino, G Giordano… - Expert Opinion on …, 2024 - Taylor & Francis
Introduction With the increasing incidence and prevalence of neurological disorders
globally, there is a paramount need for new pharmacotherapies. BBB effectively protects the …

[HTML][HTML] Nitrile-based peptoids as cysteine protease inhibitors

L Alves, DA Santos, R Cendron, FR Rocho… - Bioorganic & Medicinal …, 2021 - Elsevier
Peptidomimetics of the class of dipeptidyl nitrile analog peptoids were synthesized as
inhibitors of mammalian cysteine proteases of the papain superfamily. The dipeptidyl nitrile …

Moringa oleifera extract promotes apoptosis-like death in Toxoplasma gondii tachyzoites in vitro

L Nishi, RA da Silva Sanfelice, BT da Silva Bortoleti… - Parasitology, 2021 - cambridge.org
Toxoplasma gondii is the causative agent of toxoplasmosis, and an important problem of
public health. The current treatment for toxoplasmosis is the combination of pyrimethamine …

A High-Throughput Amenable Dual Luciferase System for Measuring Toxoplasma gondii Bradyzoite Viability after Drug Treatment

D Smith, M Lunghi, EB Olafsson, O Hatton… - Analytical …, 2022 - ACS Publications
It is estimated that more than 2 billion people are chronically infected with the intracellular
protozoan parasite Toxoplasma gondii (T. gondii). Despite this, there is currently no vaccine …

Lipophilic bisphosphonates reduced cyst burden and ameliorated hyperactivity of mice chronically infected with Toxoplasma gondii

MA Sleda, ZF Pitafi, WZ Song, E Oldfield, SNJ Moreno - Mbio, 2024 - journals.asm.org
The current treatments for toxoplasmosis are only active against fast-growing tachyzoites,
present in acute infections, with little effect on slow-growing bradyzoites within tissue cysts …

The Brazilian Toxoplasma gondii strain BRI caused greater inflammation and impairment in anxiogenic behavior in mice, which was reverted by rosuvastatin …

FF Evangelista, P de Laet Sant'Ana, WC Ferreira… - Parasitology …, 2024 - Springer
This study aimed to investigate the effect of rosuvastatin treatment on anxiety-related
behavior and short-and long-term memory impairment in mice infected with acute RH and …