Special Issue "Drug Candidates for the Treatment of Infectious Diseases"

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 29 April 2022.

Special Issue Editors

Prof. Dr. Jean Leandro dos Santos
E-Mail Website
Guest Editor
School of Pharmaceutical Science, State University of São Paulo (UNESP), São Paulo, Brazil
Interests: new drugs; drug design; drug discovery; infectious disease; medicinal chemistry
Prof. Dr. Chung Man Chin
E-Mail Website
Guest Editor
1. School of Pharmaceutical Science, State University of São Paulo (UNESP), São Paulo, Brazil
2. School of Medicine, Union of the Colleges of the Great Lakes (UNILAGO), SJRP, São Paulo, Brazil
Interests: new drugs; drug design; drug discovery; infectious disease; medicinal chemistry

Special Issue Information

Dear Colleagues,

Infectious diseases include a variety of disorders caused by parasites, bacteria, viruses, fungi, or parasites that affect millions of people worldwide. Such diseases still figure as one of the main causes of death, mainly in low-income countries, according to the World Health Organization. For some of them, the fatality rate is still high, and the treatment options remain scarce. Although scientific milestones have been achieved in the last few decades, concerns about efficacy and safety for some treatments demand efforts to discover new therapeutic agents. Moreover, due to the emergence of resistance to available drugs, it is necessary to establish medium and short-term strategies that can mitigate all those diseases. Articulated actions involving public–private partnerships seem to be one possible path to overcome the barriers found in the drug development process, mainly for neglected diseases. The COVID-19 pandemic has shown the world how articulated strategies can work by accelerating the process of discovering new therapeutic agents. In this special edition, with a focus on discovering new drug candidates for the treatment of infectious diseases, we aim to publicize the research advances that are making it possible to establish strategies to search for new anti-infectious agents—small molecules or biologics—as well as new approaches to discover potential drug candidates.

Prof. Dr. Jean Leandro dos Santos
Prof. Dr. Chung Man Chin
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2000 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • new drugs
  • drug design
  • drug discovery
  • infectious disease
  • viral infections
  • bacterial infections
  • fungal infections
  • parasitic infections
  • treatment
  • drug candidates

Published Papers (3 papers)

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Research

Article
Computational and Biological Evaluation of β-Adrenoreceptor Blockers as Promising Bacterial Anti-Virulence Agents
Pharmaceuticals 2022, 15(2), 110; https://0-doi-org.brum.beds.ac.uk/10.3390/ph15020110 - 18 Jan 2022
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Abstract
Bacterial resistance to antibiotics is an increasing public health threat as it has the potential to affect people at any stage of life, as well as veterinary. Various approaches have been proposed to counteract the bacterial resistance development. Tackling bacterial virulence is one [...] Read more.
Bacterial resistance to antibiotics is an increasing public health threat as it has the potential to affect people at any stage of life, as well as veterinary. Various approaches have been proposed to counteract the bacterial resistance development. Tackling bacterial virulence is one of the most promising approaches that confer several merits. The bacterial virulence is mainly regulated by a communication system known as quorum sensing (QS) system. Meanwhile, bacteria can sense the adrenergic hormones and eavesdrops on the host cells to establish their infection, adrenergic hormones were shown to enhance the bacterial virulence. In this study, β-adrenoreceptor blockers were proposed not only to stop bacterial espionage on our cells but also as inhibitors to the bacterial QS systems. In this context, a detailed in silico study has been conducted to evaluate the affinities of twenty-two β-blockers to compete on different structural QS receptors. Among the best docked and thermodynamically stable β-blockers; atenolol, esmolol, and metoprolol were subjected to further in vitro and in vivo investigation to evaluate their anti-QS activities against Chromobacterium violaceum, Pseudomonas aeruginosa and Salmonella typhimurium. The three tested β-blockers decreased the production of QS-controlled C. violaceum, and the formation of biofilm by P. aeruginosa and S. typhimurium. Additionally, the tested β-blockers down-regulated the P. aeruginosa QS-encoding genes and S. typhimurium sensor kinase encoding genes. Furthermore, metoprolol protected mice against P. aeruginosa and S. typhimurium. Conclusively, these investigated β-blockers are promising anti-virulence agents antagonizing adrenergic hormones induced virulence, preventing bacterial espionage, and blocking bacterial QS systems. Full article
(This article belongs to the Special Issue Drug Candidates for the Treatment of Infectious Diseases)
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Communication
Design and Synthesis of Hybrid Compounds as Epigenetic Modifiers
Pharmaceuticals 2021, 14(12), 1308; https://0-doi-org.brum.beds.ac.uk/10.3390/ph14121308 - 15 Dec 2021
Viewed by 492
Abstract
Epigenetic modifiers acting through polypharmacology mechanisms are promising compounds with which to treat several infectious diseases. Histone deacetylase (HDAC) enzymes, mainly class I, and extra-terminal bromodomains (BET) are involved in viral replication and the host response. In the present study, 10 compounds were [...] Read more.
Epigenetic modifiers acting through polypharmacology mechanisms are promising compounds with which to treat several infectious diseases. Histone deacetylase (HDAC) enzymes, mainly class I, and extra-terminal bromodomains (BET) are involved in viral replication and the host response. In the present study, 10 compounds were designed, assisted by molecular docking, to act against HDAC class I and bromodomain-4 (BRD4). All the compounds were synthesized and characterized by analytical methods. Enzymatic assays were performed using HDAC-1, -4, and -11 and BRD4. Compounds (210) inhibited both HDAC class I, mainly HDAC-1 and -2, and reduced BRD4 activity. For HDAC-1, the inhibitory effect ranged from 8 to 95%, and for HDAC-2, these values ranged from 10 to 91%. Compounds (210) decreased the BRD4 activity by up to 25%. The multi-target effects of these compounds show desirable properties that could help to combat viral infections by acting through epigenetic mechanisms. Full article
(This article belongs to the Special Issue Drug Candidates for the Treatment of Infectious Diseases)
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Article
Naphthyridine Derivatives Induce Programmed Cell Death in Naegleria fowleri
Pharmaceuticals 2021, 14(10), 1013; https://0-doi-org.brum.beds.ac.uk/10.3390/ph14101013 - 01 Oct 2021
Viewed by 549
Abstract
Primary amoebic encephalitis (PAM) caused by the opportunistic pathogen Naegleria fowleri is characterized as a rapid and lethal infection of the brain which ends in the death of the patient in more than 90% of the reported cases. This amoeba thrives in warm [...] Read more.
Primary amoebic encephalitis (PAM) caused by the opportunistic pathogen Naegleria fowleri is characterized as a rapid and lethal infection of the brain which ends in the death of the patient in more than 90% of the reported cases. This amoeba thrives in warm water bodies and causes infection after individuals perform risky activities such as splashing or diving, mostly in non-treated water bodies such as lakes and ponds. Moreover, the infection progresses very fast and no fully effective molecules have currently been found to treat PAM. In this study, naphthyridines fused with chromenes or chromenones previously synthetized by the group were tested in vitro against the trophozoite stage of two strains of N. fowleri. In addition, the most active molecule was evaluated in order to check the induction of programmed cell death (PCD) in the treated amoebae. Compound 3 showed good anti-Naegleria activity (61.45 ± 5.27 and 76.61 ± 10.84 µM, respectively) against the two different strains (ATCC® 30808 and ATCC® 30215) and a good selectivity compared to the cytotoxicity values (>300 µM). In addition, it was able to induce PCD, causing DNA condensation, damage at the cellular membrane, reduction in mitochondrial membrane potential and ATP levels, and ROS generation. Hence, naphthyridines fused with chromenes or chromenones could be potential therapeutic agents against PAM in the near future. Full article
(This article belongs to the Special Issue Drug Candidates for the Treatment of Infectious Diseases)
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