Chapter 1. Polyamine Drug Discovery: Synthetic Approaches to Therapeutic Modulators of Polyamine Metabolism

2011 ◽  
pp. 1-27
Author(s):  
Patrick M. Woster
Keyword(s):  
Drug Discovery ◽  
Polyamine Metabolism ◽  
Synthetic Approaches

scholarly journals Synthetic approaches and pharmaceutical applications of chloro-containing molecules for drug discovery: A critical review

2019 ◽  
Vol 173 ◽  
pp. 117-153 ◽  
Author(s):  
Wan-Yin Fang ◽  
L. Ravindar ◽  
K.P. Rakesh ◽  
H.M. Manukumar ◽  
C.S. Shantharam ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Critical Review ◽  
Pharmaceutical Applications ◽  
Synthetic Approaches

scholarly journals Enduracididine, a rare amino acid component of peptide antibiotics: Natural products and synthesis

2016 ◽  
Vol 12 ◽  
pp. 2325-2342 ◽  
Author(s):  
Darcy J Atkinson ◽  
Briar J Naysmith ◽  
Daniel P Furkert ◽  
Margaret A Brimble
Keyword(s):  
Natural Products ◽  
Amino Acid ◽  
Drug Discovery ◽  
Peptide Antibiotic ◽  
Peptide Antibiotics ◽  
Global Public Health ◽  
Development Of Resistance ◽  
Wide Range ◽  
Imminent Threat ◽  
Synthetic Approaches

Rising resistance to current clinical antibacterial agents is an imminent threat to global public health and highlights the demand for new lead compounds for drug discovery. One such potential lead compound, the peptide antibiotic teixobactin, was recently isolated from an uncultured bacterial source, and demonstrates remarkably high potency against a wide range of resistant pathogens without apparent development of resistance. A rare amino acid residue component of teixobactin, enduracididine, is only known to occur in a small number of natural products that also possess promising antibiotic activity. This review highlights the presence of enduracididine in natural products, its biosynthesis together with a review of analogues of enduracididine. Reported synthetic approaches to the cyclic guanidine structure of enduracididine are discussed, illustrating the challenges encountered to date in the development of efficient synthetic routes to facilitate drug discovery efforts inspired by the discovery of teixobactin.

scholarly journals 1,2,3-Triazoles: Synthesis and Biological Application

2020 ◽  
Author(s):  
Abdul Aziz Ali
Keyword(s):  
Drug Discovery ◽  
Supramolecular Chemistry ◽  
Organic Synthesis ◽  
Chemical Biology ◽  
Materials Science ◽  
Biological Activities ◽  
Fluorescent Imaging ◽  
Polymer Chemistry ◽  
Privileged Structure ◽  
Synthetic Approaches

Among nitrogen-containing heterocyclic compounds, 1,2,3-triazoles are privileged structure motif and received a great deal of attention in academics and industry. Even though absent in nature, 1,2,3-triazoles have found broad applications in drug discovery, organic synthesis, polymer chemistry, supramolecular chemistry, bioconjugation, chemical biology, fluorescent imaging, and materials science. Therefore, the development of facile and straightforward methodology for the synthesis of 1,2,3-triazoles is of noteworthy interest. In this study, emphasis will be given to numerous synthetic approaches for the synthesis of 1,2,3-triazoles, especially the popular click chemistry approach. Furthermore, several biological activities of this promising heterocycle will also be discussed.

Chapter 1: Same brain, new decade: Challenges in CNS drug discovery in the postgenomic, proteomic era

2001 ◽  
pp. 1-10 ◽  
Author(s):  
Michael Williams ◽  
Joseph T. Coyle ◽  
Sanober Shaikh ◽  
Michael W. Decker
Keyword(s):  
Drug Discovery

The Thiol-polyamine Metabolism of Trypanosoma cruzi: Molecular Targets and Drug Repurposing Strategies

2019 ◽  
Vol 26 (36) ◽  
pp. 6614-6635 ◽  
Author(s):  
Alan Talevi ◽  
Carolina Carrillo ◽  
Marcelo Comini
Keyword(s):  
Drug Discovery ◽  
Trypanosoma Cruzi ◽  
Rational Design ◽  
Biological Activities ◽  
Public Health Problem ◽  
Drug Repurposing ◽  
Polyamine Metabolism ◽  
Pharmacological Intervention ◽  
Mammalian Host ◽  
Essential Components

Chagas´ disease continues to be a challenging and neglected public health problem in many American countries. The etiologic agent, Trypanosoma cruzi, develops intracellularly in the mammalian host, which hinders treatment efficacy. Progress in the knowledge of parasite biology and host-pathogen interaction has not been paralleled by the development of novel, safe and effective therapeutic options. It is then urgent to seek for novel therapeutic candidates and to implement drug discovery strategies that may accelerate the discovery process. The most appealing targets for pharmacological intervention are those essential for the pathogen and, whenever possible, absent or significantly different from the host homolog. The thiol-polyamine metabolism of T. cruzi offers interesting candidates for a rational design of selective drugs. In this respect, here we critically review the state of the art of the thiolpolyamine metabolism of T. cruzi and the pharmacological potential of its components. On the other hand, drug repurposing emerged as a valid strategy to identify new biological activities for drugs in clinical use, while significantly shortening the long time and high cost associated with de novo drug discovery approaches. Thus, we also discuss the different drug repurposing strategies available with a special emphasis in their applications to the identification of drug candidates targeting essential components of the thiol-polyamine metabolism of T. cruzi.

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