scholarly journals Diversity-Oriented Synthesis Yields a New Drug Lead for Treatment of Chagas Disease

2014 ◽  
Vol 5 (2) ◽  
pp. 149-153 ◽  
Author(s):  
Sivaraman Dandapani ◽  
Andrew R. Germain ◽  
Ivan Jewett ◽  
Sebastian le Quement ◽  
Jean-Charles Marie ◽  
...  
2019 ◽  
Vol 22 (8) ◽  
pp. 509-520
Author(s):  
Cauê B. Scarim ◽  
Chung M. Chin

Background: In recent years, there has been an improvement in the in vitro and in vivo methodology for the screening of anti-chagasic compounds. Millions of compounds can now have their activity evaluated (in large compound libraries) by means of high throughput in vitro screening assays. Objective: Current approaches to drug discovery for Chagas disease. Method: This review article examines the contribution of these methodological advances in medicinal chemistry in the last four years, focusing on Trypanosoma cruzi infection, obtained from the PubMed, Web of Science, and Scopus databases. Results: Here, we have shown that the promise is increasing each year for more lead compounds for the development of a new drug against Chagas disease. Conclusion: There is increased optimism among those working with the objective to find new drug candidates for optimal treatments against Chagas disease.


2012 ◽  
Vol 6 (11) ◽  
pp. e1870 ◽  
Author(s):  
Maria Terezinha Bahia ◽  
Isabel Mayer de Andrade ◽  
Tassiane Assíria Fontes Martins ◽  
Álvaro Fernando da Silva do Nascimento ◽  
Lívia de Figueiredo Diniz ◽  
...  

2007 ◽  
Vol 6 (2) ◽  
pp. 113-113
Author(s):  
Alexandra Flemming
Keyword(s):  
New Drug ◽  

2018 ◽  
Vol 67 (29) ◽  
pp. 803-805 ◽  
Author(s):  
Barbara L. Herwaldt ◽  
Cindy P. Dougherty ◽  
Christopher K. Allen ◽  
Julian P. Jolly ◽  
Megan N. Brown ◽  
...  

2007 ◽  
Vol 5 (3) ◽  
pp. 165-165
Author(s):  
Alexandra Flemming
Keyword(s):  
New Drug ◽  

2021 ◽  
Author(s):  
Xi-Chao Wang ◽  
Hao-Ran Wang ◽  
Xiufang Xu ◽  
Dongbing Zhao

Investigations of the sila-8-membered ring fused biaryls are of important significance for the discovery of new drug lead compounds. However, such compounds are still unknown due to the synthetic challenge. Herein we describe the chemo- and regio-selective cross-dimerization of 5-membered palladacycles with silacyclobutanes enabled by Pd-catalytic conditions, which constitutes an expedient ring expansion route to the sila-8-membered ring fused biaryl skeletons.


2021 ◽  
Vol 12 ◽  
Author(s):  
Federico Serral ◽  
Florencia A. Castello ◽  
Ezequiel J. Sosa ◽  
Agustín M. Pardo ◽  
Miranda Clara Palumbo ◽  
...  

Decades of successful use of antibiotics is currently challenged by the emergence of increasingly resistant bacterial strains. Novel drugs are urgently required but, in a scenario where private investment in the development of new antimicrobials is declining, efforts to combat drug-resistant infections become a worldwide public health problem. Reasons behind unsuccessful new antimicrobial development projects range from inadequate selection of the molecular targets to a lack of innovation. In this context, increasingly available omics data for multiple pathogens has created new drug discovery and development opportunities to fight infectious diseases. Identification of an appropriate molecular target is currently accepted as a critical step of the drug discovery process. Here, we review how diverse layers of multi-omics data in conjunction with structural/functional analysis and systems biology can be used to prioritize the best candidate proteins. Once the target is selected, virtual screening can be used as a robust methodology to explore molecular scaffolds that could act as inhibitors, guiding the development of new drug lead compounds. This review focuses on how the advent of omics and the development and application of bioinformatics strategies conduct a “big-data era” that improves target selection and lead compound identification in a cost-effective and shortened timeline.


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