Nonclassical routes for amide bond formation

RM De Figueiredo, JS Suppo, JM Campagne - Chemical reviews, 2016 - ACS Publications
The present review offers an overview of nonclassical (eg, with no pre-or in situ activation of
a carboxylic acid partner) approaches for the construction of amide bonds. The review aims …

Trypanosoma cruzi targets for new chemotherapeutic approaches

MNC Soeiro, SL de Castro - Expert Opinion on Therapeutic Targets, 2009 - Taylor & Francis
Background: Strategies for development of anti-parasite chemotherapy involve identification
of active principles of plants, investigation of drugs already licensed for other pathologies, or …

Vinyl sulfones as antiparasitic agents and a structural basis for drug design

ID Kerr, JH Lee, CJ Farady, R Marion, M Rickert… - Journal of Biological …, 2009 - ASBMB
Cysteine proteases of the papain superfamily are implicated in a number of cellular
processes and are important virulence factors in the pathogenesis of parasitic disease …

Inhibition of rhodesain as a novel therapeutic modality for human African trypanosomiasis

R Ettari, L Tamborini, IC Angelo, N Micale… - Journal of Medicinal …, 2013 - ACS Publications
Rhodesain, a cathepsin L-like cysteine protease of T. brucei rhodesiense, is considered a
potential target for the treatment of human African trypanosomiasis. Recent findings have …

A carbonate-forming Baeyer-Villiger monooxygenase

Y Hu, D Dietrich, W Xu, A Patel, JAJ Thuss… - Nature chemical …, 2014 - nature.com
Despite the remarkable versatility displayed by flavin-dependent monooxygenases (FMOs)
in natural product biosynthesis, one notably missing activity is the oxidative generation of …

Cruzain inhibitors: efforts made, current leads and a structural outlook of new hits

K Martinez-Mayorga, KG Byler… - Drug Discovery …, 2015 - Elsevier
Highlights•SAR and docking studies should be interpreted considering the possibility of
aggregation.•SAR does not necessarily imply a specific binding interaction.•Neutral …

Synthesis and structure-activity relationship studies of cruzain and rhodesain inhibitors

DA Rocha, EB Silva, IS Fortes, MS Lopes… - European Journal of …, 2018 - Elsevier
Abstract Chagas disease and Human African trypanosomiasis (HAT) are important public
health issues in Latin American and sub-Saharan African countries, respectively, and are …

Design, synthesis and biological evaluation of novel thiosemicarbazones as cruzipain inhibitors

G Jasinski, E Salas-Sarduy, D Vega, L Fabian… - European Journal of …, 2023 - Elsevier
Based on the activity of 23 TSCs on CZ taken from the literature, we have developed a
QSAR model for predicting the activity of TSCs. New TSCs were designed and then tested …

Quantum mechanics/molecular mechanics studies of the mechanism of cysteine proteases inhibition by dipeptidyl nitroalkenes

K Arafet, FV González, V Moliner - Chemistry–A European …, 2020 - Wiley Online Library
In this work a computational study of the mechanism of inhibition of cruzain, rhodesain, and
cathepsin L cysteine proteases by the dipeptidyl nitroalkene Cbz‐Phe‐Ala‐CH= CH‐NO2 …

Stairway to heaven or hell? Perspectives and limitations of Chagas disease chemotherapy

K Salomao… - Current Topics in …, 2016 - ingentaconnect.com
In this review, we intend to provide a general view of the evolution of experimental studies in
the area of chemotherapy for Chagas disease. We can follow the process of drug …