Novel scaffolds for inhibition of Cruzipain identified from high-throughput screening of anti-kinetoplastid chemical boxes

E Salas-Sarduy, LU Landaburu, J Karpiak… - Scientific reports, 2017 - nature.com
Abstract American Trypanosomiasis or Chagas disease is a prevalent, neglected and
serious debilitating illness caused by the kinetoplastid protozoan parasite Trypanosoma …

Non-peptidic cruzain inhibitors with trypanocidal activity discovered by virtual screening and in vitro assay

HJ Wiggers, JR Rocha, WB Fernandes… - PLoS neglected …, 2013 - journals.plos.org
A multi-step cascade strategy using integrated ligand-and target-based virtual screening
methods was developed to select a small number of compounds from the ZINC database to …

Development of α-keto-based inhibitors of cruzain, a cysteine protease implicated in Chagas disease

Y Choe, LS Brinen, MS Price, JC Engel… - Bioorganic & medicinal …, 2005 - Elsevier
Trypanosoma cruzi, a protozoan parasite, is the causative agent of Chagas disease, a major
cause of cardiovascular disease in many Latin American countries. There is an urgent need …

Nonpeptidic tetrafluorophenoxymethyl ketone cruzain inhibitors as promising new leads for Chagas disease chemotherapy

K Brak, ID Kerr, KT Barrett, N Fuchi… - Journal of medicinal …, 2010 - ACS Publications
A century after discovering that the Trypanosoma cruzi parasite is the etiological agent of
Chagas disease, treatment is still plagued by limited efficacy, toxicity, and the emergence of …

On the intrinsic reactivity of highly potent trypanocidal cruzain inhibitors

V Bonatto, PHJ Batista, L Cianni, D De Vita… - RSC Medicinal …, 2020 - pubs.rsc.org
The cysteine protease cruzipain is considered to be a validated target for therapeutic
intervention in the treatment of Chagas disease. Hence, peptidomimetic cruzipain inhibitors …

Cruzipain: an update on its potential as chemotherapy target against the human pathogen Trypanosoma cruzi

MH Branquinha, SSC Oliveira… - Current medicinal …, 2015 - ingentaconnect.com
Chagas' disease is one of the most impactful and prevalent neglected tropical diseases in
the Americas, specially affecting the poor and underdeveloped areas in Latin America …

Structure-based discovery of novel cruzain inhibitors with distinct trypanocidal activity profiles

VC Santos, PG Leite, LH Santos, PG Pascutti… - European Journal of …, 2023 - Elsevier
Over 110 years after the first formal description of Chagas disease, the trypanocidal drugs
thus far available have limited efficacy and several side effects. This encourages the search …

Synthesis, Biological Evaluation, and Structure–Activity Relationships of Potent Noncovalent and Nonpeptidic Cruzain Inhibitors as Anti-Trypanosoma cruzi Agents

RS Ferreira, MA Dessoy, I Pauli… - Journal of medicinal …, 2014 - ACS Publications
The development of cruzain inhibitors has been driven by the urgent need to develop novel
and more effective drugs for the treatment of Chagas' disease. Herein, we report the lead …

Amidines bearing benzofuroxan or benzimidazole 1, 3-dioxide core scaffolds as Trypanosoma cruzi-inhibitors: structural basis for their interactions with cruzipain

A Merlino, D Benitez, NE Campillo, JA Páez… - …, 2012 - pubs.rsc.org
Trypanosoma cruzi, the causative agent of Chagas' disease, affects tens of millions of South
Americans. One of the most studied T. cruzi-biomolecules as a target for drug development …

Novel cruzain inhibitors for the treatment of Chagas' disease

KE Rogers, H Keränen, JD Durrant… - Chemical biology & …, 2012 - Wiley Online Library
The protozoan parasite Trypanosoma cruzi, the etiological agent of Chagas' disease, affects
millions of individuals and continues to be an important global health concern. The poor …