Covalent Inhibitors for Neglected Diseases: An Exploration of Novel Therapeutic Options

ETM Alves, FG Pernichelle, LA Nascimento… - Pharmaceuticals, 2023 - mdpi.com
Neglected diseases, primarily found in tropical regions of the world, present a significant
challenge for impoverished populations. Currently, there are 20 diseases considered …

Targeting eukaryotic proteases for natural products-based drug development

FH Al-Awadhi, H Luesch - Natural product reports, 2020 - pubs.rsc.org
Covering: up to April 2020 Proteases are involved in the regulation of many physiological
processes. Their overexpression and dysregulated activity are linked to diseases such as …

Coumarin-based derivatives targeting Trypanosoma cruzi cruzain and Trypanosoma brucei cathepsin L-like proteases

JA Nunes, FN da Silva, EB da Silva… - New Journal of …, 2023 - pubs.rsc.org
The protozoa, Trypanosoma cruzi (etiological agent of Chagas diseases–also named
American trypanosomiasis) and T. brucei (causative agent of human African …

Nature-Inspired Gallinamides Are Potent Antischistosomal Agents: Inhibition of the Cathepsin B1 Protease Target and Binding Mode Analysis

P Spiwoková, M Horn, J Fanfrlík, A Jílková… - ACS Infectious …, 2024 - ACS Publications
Schistosomiasis, caused by a parasitic blood fluke of the genus Schistosoma, is a global
health problem for which new chemotherapeutic options are needed. We explored the …

Potential of bioactive molecules from photosynthetic microorganisms on Leishmania spp.: A review

SSS da Silva, AF de Andrade, M de Paiva-Cavalcanti… - Algal Research, 2023 - Elsevier
Leishmaniasis is an infectious disease caused by protozoan parasites from the Leishmania
genus, representing a significant global public health issue that affects thousands of …

Marine Pharmacology in 2019–2021: Marine Compounds with Antibacterial, Antidiabetic, Antifungal, Anti-Inflammatory, Antiprotozoal, Antituberculosis and Antiviral …

A Mayer, VA Mayer, M Swanson-Mungerson… - Marine Drugs, 2024 - mdpi.com
The current 2019–2021 marine pharmacology literature review provides a continuation of
previous reviews covering the period 1998 to 2018. Preclinical marine pharmacology …

Metabolomic Analysis and Antiviral Screening of a Marine Algae Library Yield Jobosic Acid (2, 5-Dimethyltetradecanoic Acid) as a Selective Inhibitor of SARS-CoV-2

ML Matos-Hernández, R Samples, G Dyer… - Journal of Natural …, 2024 - ACS Publications
Current small-molecule-based SARS-CoV-2 treatments have limited global accessibility and
pose the risk of inducing viral resistance. Therefore, a marine algae and cyanobacteria …

First Total Synthesis and Structure–Activity Relationship of Iheyamide A, an Antitrypanosomal Linear Peptide Isolated from a Dapis sp. Marine Cyanobacterium

A Iwasaki, K Teranuma, N Kurisawa… - Journal of Natural …, 2021 - ACS Publications
Iheyamide A (1) is an antitrypanosomal linear peptide isolated from a Dapis sp. marine
cyanobacterium by our group in 2020, and based on structure–activity relationships of its …

Mapping the S1 and S1'subsites of cysteine proteases with new dipeptidyl nitrile inhibitors as trypanocidal agents

L Cianni, C Lemke, E Gilberg, C Feldmann… - PLoS neglected …, 2020 - journals.plos.org
The cysteine protease cruzipain is considered to be a validated target for therapeutic
intervention in the treatment of Chagas disease. A series of 26 new compounds were …

Structure-based discovery of thiosemicarbazones as SARS-CoV-2 main protease inhibitors

VG Maltarollo, EB da Silva, T Kronenberger… - Future Medicinal …, 2023 - Taylor & Francis
Aim: Discovery of novel SARS-CoV-2 main protease (Mpro) inhibitors using a structure-
based drug discovery strategy. Materials & methods: Virtual screening employing covalent …