Structural Optimization and Biological Activity of Pyrazole Derivatives: Virtual Computational Analysis, Recovery Assay and 3D Culture Model as Potential Predictive Tools of Effectiveness against Trypanosoma cruzi

Three dimensional cultivation increases chemo- and radioresistance of colorectal cancer cell lines

(2021) Jana Koch et al.   PLoS One

New regimens of benznidazole monotherapy and in combination with fosravuconazole for treatment of Chagas disease (BENDITA): a phase 2, double-blind, randomised trial

(2021) Faustino Torrico et al.   LANCET INFECTIOUS DISEASES

Transmigration of Trypanosoma cruzi trypomastigotes through 3D cultures resembling a physiological environment

(2020) Matías Exequiel Rodríguez et al.   CELLULAR MICROBIOLOGY

Synthesis of Pyrazole-Carboxamides and Pyrazole-Carboxylic Acids Derivatives: Simple Methods to Access Powerful Building Blocks

(2020) Byanca Silva Ferreira et al.   LETTERS IN ORGANIC CHEMISTRY

Effect of Posaconazole in an in vitro model of cardiac fibrosis induced by Trypanosoma cruzi

(2020) Lindice Mitie Nisimura et al.   MOLECULAR AND BIOCHEMICAL PARASITOLOGY

A Convenient Synthesis of Pyrazole‐imidazoline Derivatives by Microwave Irradiation

(2019) Getúlio de S. Rosa et al.   JOURNAL OF HETEROCYCLIC CHEMISTRY

Chagas Disease: From Discovery to a Worldwide Health Problem

(2019) Kárita Cláudia Freitas Lidani et al.   Frontiers in Public Health

Discovery of Pyrrolo[2,3-b]pyridine (1,7-Dideazapurine) Nucleoside Analogues as Anti-Trypanosoma cruzi Agents

(2019) Cai Lin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Potent N-Ethylurea Pyrazole Derivatives as Dual Inhibitors of Trypanosoma brucei and Trypanosoma cruzi

(2019) Swapna Varghese et al.   ACS Medicinal Chemistry Letters

Flexible 3D Cell-Based Platforms for the Discovery and Profiling of Novel Drugs Targeting Plasmodium Hepatic Infection

(2019) Francisca Arez et al.   ACS Infectious Diseases

Using Physicochemical Measurements to Influence Better Compound Design

(2019) Shenaz B. Bunally et al.   SLAS Discovery

Synthesis, structure-activity relationship and trypanocidal activity of pyrazole-imidazoline and new pyrazole-tetrahydropyrimidine hybrids as promising chemotherapeutic agents for Chagas disease

(2019) M.E. Monteiro et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Mapping benznidazole resistance in trypanosomatids and exploring evolutionary histories of nitroreductases and ABCG transporter protein sequences

(2019) Pamela O. Petravicius et al.   ACTA TROPICA

Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration

(2018) Ludmila Ferreira de Almeida Fiuza et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Treatment of adult chronic indeterminate Chagas disease with benznidazole and three E1224 dosing regimens: a proof-of-concept, randomised, placebo-controlled trial

(2018) Faustino Torrico et al.   LANCET INFECTIOUS DISEASES

3-pyridyl inhibitors with novel activity against Trypanosoma cruzi reveal in vitro profiles can aid prediction of putative cytochrome P450 inhibition

(2018) Melissa L. Sykes et al.   Scientific Reports

Development of Trypanosoma cruzi in vitro assays to identify compounds suitable for progression in Chagas’ disease drug discovery

(2018) Lorna M. MacLean et al.   PLoS Neglected Tropical Diseases

Three-Dimensional in Vitro Cell Culture Models in Drug Discovery and Drug Repositioning

(2018) Sigrid A. Langhans   Frontiers in Pharmacology

admetSAR 2.0: web-service for prediction and optimization of chemical ADMET properties

(2018) Hongbin Yang et al.   BIOINFORMATICS

Update on drug development targeting parasite cysteine proteases

(2018) James H. McKerrow   PLoS Neglected Tropical Diseases

Chagas disease in Europe: A review for the internist in the globalized world

(2017) Spinello Antinori et al.   European Journal of Internal Medicine

Benznidazole and Posaconazole in Eliminating Parasites in Asymptomatic  T. Cruzi Carriers

(2017) Carlos A. Morillo et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Repositioning FDA Drugs as Potential Cruzain Inhibitors from Trypanosoma cruzi: Virtual Screening, In Vitro and In Vivo Studies

(2017) Isidro Palos et al.   MOLECULES

Simple dialkyl pyrazole-3,5-dicarboxylates show in vitro and in vivo activity against disease-causing trypanosomatids

(2017) FELIPE REVIRIEGO et al.   PARASITOLOGY

SwissADME: a free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules

(2017) Antoine Daina et al.   Scientific Reports

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

(2017) Emir Salas-Sarduy et al.   Scientific Reports

New carbohydrazide derivatives of 1H-pyrazolo[3,4-b]pyridine and trypanocidal activity

(2016) RAQUEL R.S. SALVADOR et al.   ANAIS DA ACADEMIA BRASILEIRA DE CIENCIAS

DataWarrior: An Open-Source Program For Chemistry Aware Data Visualization And Analysis

(2015) Thomas Sander et al.   Journal of Chemical Information and Modeling

Randomized Trial of Benznidazole for Chronic Chagas’ Cardiomyopathy

(2015) Carlos A. Morillo et al.   NEW ENGLAND JOURNAL OF MEDICINE

FAF-Drugs3: a web server for compound property calculation and chemical library design

(2015) David Lagorce et al.   NUCLEIC ACIDS RESEARCH

Randomized Trial of Posaconazole and Benznidazole for Chronic Chagas' Disease

(2014) Israel Molina et al.   NEW ENGLAND JOURNAL OF MEDICINE

Reversible Cysteine Protease Inhibitors Show Promise for a Chagas Disease Cure

(2013) Momar Ndao et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Synthesis and activity of novel tetrazole compounds and their pyrazole-4-carbonitrile precursors against Leishmania spp

(2013) Jéssica V. Faria et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

American Trypanosomiasis (Chagas Disease)

(2012) Anis Rassi et al.   INFECTIOUS DISEASE CLINICS OF NORTH AMERICA

An Efficient Synthesis of New 5-(1-Aryl-1H-pyrazole-4-yl)-1H-tetrazoles from 1-Aryl-1H-pyrazole-4-carbonitrilesvia[3 + 2] Cycloaddition Reaction

(2012) Maurício S. dos Santos et al.   JOURNAL OF HETEROCYCLIC CHEMISTRY

Methyl Effects on Protein–Ligand Binding

(2012) Cheryl S. Leung et al.   JOURNAL OF MEDICINAL CHEMISTRY

In Vitro and in Vivo Trypanosomicidal Activity of Pyrazole-Containing Macrocyclic and Macrobicyclic Polyamines: Their Action on Acute and Chronic Phases of Chagas Disease

(2012) Manuel Sánchez-Moreno et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bioluminescent imaging of Trypanosoma cruzi infection in Rhodnius prolixus

(2012) Cristina Henriques et al.   Parasites & Vectors

Synthesis and antileishmanial evaluation of 1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-1H-pyrazole derivatives

(2011) Maurício S. dos Santos et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The Trypanosoma cruzi Protease Cruzain Mediates Immune Evasion

(2011) Patricia S. Doyle et al.   PLoS Pathogens

Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease

(2010) Christian Beaulieu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Chagas disease

(2010) Anis Rassi et al.   LANCET

Pharmacological Promiscuity: Dependence on Compound Properties and Target Specificity in a Set of Recent Roche Compounds

(2009) Jens-Uwe Peters et al.   ChemMedChem

Fibrosis and Hypertrophy Induced byTrypanosoma cruziin a Three‐Dimensional Cardiomyocyte‐Culture System

(2008) Luciana Ribeiro Garzoni et al.   JOURNAL OF INFECTIOUS DISEASES