4.4 Review

The Importance of the Piperazine Ring for the Development of Trypanomicide Compounds

相关参考文献

注意:仅列出部分参考文献,下载原文获取全部文献信息。
Article Pharmacology & Pharmacy

Optimization of physicochemical properties is a strategy to improve drug-likeness associated with activity: Novel active and selective compounds against Trypanosoma cruzi

Marina T. Varela et al.

Summary: This study aimed to modify the core structure of the LINS03 series compounds in order to achieve a balance between favorable physicochemical properties and biological activity. The addition of water-solubilizing groups and privileged substructures greatly improved the drug-likeness of the compounds, increased potency, and maintained selectivity towards the parasite.

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES (2022)

Article Biochemistry & Molecular Biology

Trypanosoma cruzi nitroreductase: Structural features and interaction with biological membranes

Marilia L. Cirqueira et al.

Summary: Due to its severe burden and geographic distribution, Chagas disease has a significant social and economic impact on low-income countries. This study aims to understand the role of TcNTR in the basic parasite biology, investigate its potential as a drug target, and contribute to the fight against neglected tropical diseases. The results showed that TcNTR interacts with membranes, with a preference for those containing cardiolipin, and a 23-residue long insertion is involved in enzyme specificity and protein-membrane interaction.

INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES (2022)

Article Chemistry, Medicinal

A new chemotype with promise against Trypanosoma cruzi

Xiaofang Wang et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2020)

Review Pharmacology & Pharmacy

An Overview of Piperazine Scaffold as Promising Nucleus for Different Therapeutic Targets

Anjali Sharma et al.

CURRENT PHARMACEUTICAL DESIGN (2020)

Article Biochemistry & Molecular Biology

Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation

Rocio Paucar et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2019)

Article Chemistry, Medicinal

Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi

Ruben Martin-Escolano et al.

JOURNAL OF MEDICINAL CHEMISTRY (2018)

Review Biochemistry & Molecular Biology

Seven Year Itch: Pan-Assay Interference Compounds (PAINS) in 2017-Utility and Limitations

Jonathan B. Baell et al.

ACS CHEMICAL BIOLOGY (2018)

Article Biochemistry & Molecular Biology

Application of bioisosterism in design of the semicarbazone derivatives as cruzain inhibitors: a theoretical and experimental study

Drielli G. Vital et al.

JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS (2017)

Review Chemistry, Organic

Recent Advances in Piperazine Synthesis

Kristen E. Gettys et al.

SYNTHESIS-STUTTGART (2017)

Article Chemistry, Medicinal

A comparative study of warheads for design of cysteine protease inhibitors

Daniel G. Silva et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2017)

Article Chemistry, Medicinal

Synthesis and Evaluation of Oxyguanidine Analogues of the Cysteine Protease Inhibitor WRR-483 against Cruzain

Brian D. Jones et al.

ACS MEDICINAL CHEMISTRY LETTERS (2016)

Article Chemistry, Medicinal

Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds

Maria V. Papadopoulou et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2016)

Article Chemistry, Medicinal

In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives

Elsa Moreno-Viguri et al.

JOURNAL OF MEDICINAL CHEMISTRY (2016)

Article Biochemical Research Methods

Computational and Practical Aspects of Drug Repositioning

Tudor I. Oprea et al.

ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES (2015)

Article Chemistry, Medicinal

3-Nitrotriazole-based piperazides as potent antitrypanosomal agents

Maria V. Papadopoulou et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2015)

Article Chemistry, Medicinal

Design, synthesis and biological evaluation of quinazoline derivatives as anti-trypanosomatid and anti-plasmodial agents

Cesar Mendoza-Martinez et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2015)

Article Chemistry, Medicinal

Binding Mode and Potency of N-Indolyloxopyridinyl-4-aminopropanyl-Based Inhibitors Targeting Trypanosoma cruzi CYP51

Debora F. Vieira et al.

JOURNAL OF MEDICINAL CHEMISTRY (2014)

Article Parasitology

Anti-Trypanosoma cruzi and anti-leishmanial activity by quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives

Juan Carlos Villalobos-Rocha et al.

PARASITOLOGY RESEARCH (2014)

Article Biochemistry & Molecular Biology

Novel 3-nitro-1H-1,2,4-triazole-based piperazines and 2-amino-1,3-benzothiazoles as antichagasic agents

Maria V. Papadopoulou et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2013)

Article Pharmacology & Pharmacy

Target Sites for the Design of Anti-trypanosomatid Drugs Based on the Structure of Dihydroorotate Dehydrogenase

Matheus Pinto Pinheiro et al.

CURRENT PHARMACEUTICAL DESIGN (2013)

Article Chemistry, Medicinal

Rational Development of 4-Aminopyridyl-Based Inhibitors Targeting Trypanosoma cruzi CYP51 as Anti-Chagas Agents

Jun Yong Choi et al.

JOURNAL OF MEDICINAL CHEMISTRY (2013)

Article Chemistry, Medicinal

Novel 3-Nitro-1H-1,2,4-triazole-Based Aliphatic and Aromatic Amines as Anti-Chagasic Agents

Maria V. Papadopoulou et al.

JOURNAL OF MEDICINAL CHEMISTRY (2011)

Article Parasitology

Two approaches to discovering and developing new drugs for Chagas disease

J. H. McKerrow et al.

MEMORIAS DO INSTITUTO OSWALDO CRUZ (2009)

Article Chemistry, Medicinal

Potency and selectivity of P2/P3-modified inhibitors of cysteine proteases from trypanosomes

Priyadarshini Jaishankar et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2008)

Article Chemistry, Medicinal

Naphthoquinoidal [1,2,3]-triazole, a new structural moiety active against Trypanosoma cruzi

Eufranio N. da Silva et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2008)

Article Biochemistry & Molecular Biology

Benzofuranyl 3,5-bis-polyamine derivatives as time-dependent inhibitors of trypanothione reductase

CJ Hamilton et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2003)