Recent progress on 1H-1,2,3-triazoles as potential antifungal agents

Author(s):  
Nisha Poonia ◽  
Aman Kumar ◽  
Vijay Kumar ◽  
Monika Yadav ◽  
Kashmiri Lal

: To overcome ever increasing cases of antifungal resistance and circumventing side effects and drug interactions related with currently available drugs has impelled the need to expedite the process of drug discovery and development of novel antifungals. 1,4-Disubstituted 1,2,3-triazole has gained tremendous interest in last two decades mainly because of its ease of synthesis via copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) and its broad spectrum of chemotherapeutic potential. 1,2,3-Triazole is an excellent pharmacophore which has been used as a bioisostere for obtaining libraries of new medicinally important scaffolds. The present review focus on the recent advances (2016-2021) of 1,2,3-triazole derivatives obtained by CuAAC as potential antifungal agents that may facilitate triazole based antifungal development process.

2009 ◽  
Vol 1 ◽  
pp. CMT.S2297 ◽  
Author(s):  
Jennifer L. Halsey

Nitazoxanide is a broad-spectrum agent active against several protozoa, helminths, and bacteria, including C. difficile and H. pylori. It is available as an oral tablet and suspension, both with adequate bioavailability. Nitazoxanide is associated with minimal side effects, has an acceptable safety profile, and has been classified as a pregnancy category B agent. It is 99% protein bound, which could result in drug interactions. It is the preferred agent for the treatment of Cryptospordiosis and Giardiasis in immunocompetent patients and has shown promise for the treatment of rotavirus, mild to moderate initial C. difficile infection, refractory C. difficile infection, Amoebiasis, Blastocystosis, and Taenia saginata.


2020 ◽  
Vol 10 (7) ◽  
pp. 2376 ◽  
Author(s):  
Rob C. van Wijk ◽  
Rami Ayoun Alsoud ◽  
Hans Lennernäs ◽  
Ulrika S. H. Simonsson

The increasing emergence of drug-resistant tuberculosis requires new effective and safe drug regimens. However, drug discovery and development are challenging, lengthy and costly. The framework of model-informed drug discovery and development (MID3) is proposed to be applied throughout the preclinical to clinical phases to provide an informative prediction of drug exposure and efficacy in humans in order to select novel anti-tuberculosis drug combinations. The MID3 includes pharmacokinetic-pharmacodynamic and quantitative systems pharmacology models, machine learning and artificial intelligence, which integrates all the available knowledge related to disease and the compounds. A translational in vitro-in vivo link throughout modeling and simulation is crucial to optimize the selection of regimens with the highest probability of receiving approval from regulatory authorities. In vitro-in vivo correlation (IVIVC) and physiologically-based pharmacokinetic modeling provide powerful tools to predict pharmacokinetic drug-drug interactions based on preclinical information. Mechanistic or semi-mechanistic pharmacokinetic-pharmacodynamic models have been successfully applied to predict the clinical exposure-response profile for anti-tuberculosis drugs using preclinical data. Potential pharmacodynamic drug-drug interactions can be predicted from in vitro data through IVIVC and pharmacokinetic-pharmacodynamic modeling accounting for translational factors. It is essential for academic and industrial drug developers to collaborate across disciplines to realize the huge potential of MID3.


2003 ◽  
Vol 70 (3) ◽  
pp. S73-S85 ◽  
Author(s):  
Robert S. Mansbach ◽  
Douglas E. Feltner ◽  
Lisa H. Gold ◽  
Sidney H. Schnoll

2018 ◽  
Vol 32 (5) ◽  
pp. 302-311 ◽  
Author(s):  
Elizabeth K. McClain ◽  
Yolanda Johnson-Moton ◽  
Bryan Larsen ◽  
Rebecca J. Bartlett Ellis ◽  
Eric Niederhoffer

The approach to building innovative partnerships between academia and the pharmaceutical industry has expanded to investigate collaborations that offer meaningful outcomes beyond discovery and increased productivity. This case study uses a systems thinking approach to guide the process and analyse the outcome of a partnership undertaken by one pharmaceutical company and academia. The collaborative process established three tiers of evolution over a 3-year period. The outcome was an online module–based course, entitled ‘Making Medicines: The Process of Drug Development’, that provides information about the drug discovery and development process. Both the course development and the final product serve as a useful case study of how collaboration between academia and industry might be achieved. The development process itself is proposed as an appropriate approach for building educational partnerships.


2019 ◽  
Vol 7 (6) ◽  
pp. 62-67 ◽  
Author(s):  
Amol B Deore ◽  
Jayprabha R Dhumane ◽  
Rushikesh Wagh ◽  
Rushikesh Sonawane

Drug discovery is a process which aims at identifying a compound therapeutically useful in curing and treating disease. This process involves the identification of candidates, synthesis, characterization, validation, optimization, screening and assays for therapeutic efficacy. Once a compound has shown its significance in these investigations, it will initiate the process of drug development earlier to clinical trials. New drug development process must continue through several stages in order to make a medicine that is safe, effective, and has approved all regulatory requirements. One overall theme of our article is that the process is sufficiently long, complex, and expensive so that many biological targets must be considered for every new medicine ultimately approved for clinical use and new research tools may be needed to investigate each new target.  From initial discovery to a marketable medicine is a long, challenging task. It takes about 12 - 15 years from discovery to the approved medicine and requires an investment of about US $1 billion. On an average, a million molecules screened but only a single is explored in late stage clinical trials and is finally made obtainable for patients. This article provides a brief outline of the processes of new drug discovery and development.   


2021 ◽  
Vol 9 ◽  
Author(s):  
Agnieszka Staśkiewicz ◽  
Patrycja Ledwoń ◽  
Paolo Rovero ◽  
Anna Maria Papini ◽  
Rafal Latajka

Peptidomimetics play a fundamental role in drug design due to their preferential properties regarding natural peptides. In particular, compounds possessing nitrogen-containing heterocycles have been intensively studied in recent years. The triazolyl moiety incorporation decreases the molecule susceptibility to enzymatic degradation, reduction, hydrolysis, and oxidation. In fact, peptides containing triazole rings are a typical example of peptidomimetics. They have all the advantages over classic peptides. Both efficient synthetic methods and biological activity make these systems an interesting and promising object of research. Peptide triazole derivatives display a diversity of biological properties and can be obtained via numerous synthetic strategies. In this review, we have highlighted the importance of the triazole-modified peptidomimetics in the field of drug design. We present an overview on new achievements in triazolyl-containing peptidomimetics synthesis and their biological activity as inhibitors of enzymes or against cancer, viruses, bacteria, or fungi. The relevance of above-mentioned compounds was confirmed by their comparison with unmodified peptides.


2019 ◽  
Vol 108 (1) ◽  
pp. 87-101 ◽  
Author(s):  
Stephanie Dodd ◽  
Sivacharan Kollipara ◽  
Manuel Sanchez-Felix ◽  
Hyungchul Kim ◽  
Qingshuo Meng ◽  
...  

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