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Pharmaceuticals
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Small Molecules as Antimicrobials 2022
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Small Molecules as Antimicrobials 2022

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

Deadline for manuscript submissions: closed (15 April 2023) | Viewed by 11548

Special Issue Editor

Dr. Poce Giovanna

E-Mail Website
Guest Editor
Department of Chemistry and Technology of Drugs (DCTF), Sapienza University of Rome, Rome, Italy
Interests: medicinal chemistry; drug development; antimycobacterials; antibacterials
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The World Health Organization (WHO) has announced antimicrobial resistance (AMR) as a major threat to public health. The rapid development and spread of new resistance mechanisms has made many antimicrobials useless in treating clinically ill patients. Even medical procedures such as major surgery, organ transplantation, and cancer chemotherapy have become very risky in the absence of effective antimicrobials for the prevention and treatment of infections. Therefore, there is an urgent need for new, better, and more effective antimicrobials.

We invite authors to submit original research and review articles related to up-to-date and ongoing research focusing on the development and evaluation of potential new antimicrobial agents, as well as on the investigation of improved delivery protocols of both existing and new antimicrobial agents. We aim to highlight research covering all stages of investigation, such as in silico studies, synthesis efforts, in vitro studies, and in vivo evaluations.

Potential topics include but are not limited to:

  • Development and testing of novel and effective antimicrobial agents;
  • Antimicrobial agents active against drug-resistant forms;
  • Recent advances in antimicrobial drug delivery.

Dr. Poce Giovanna
Guest Editor

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 submissions that pass pre-check are 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 2900 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

  • medicinal chemistry
  • antimycobacterials
  • antibacterials

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Published Papers (3 papers)

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Research

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16 pages, 3494 KiB  
Article
Rifampicin Enhanced Carbapenem Activity with Improved Antibacterial Effects and Eradicates Established Acinetobacter baumannii Biofilms
by Lois Chinwe Nwabor, Arnon Chukamnerd, Ozioma Forstinus Nwabor, Rattanaruji Pomwised, Supayang P. Voravuthikunchai and Sarunyou Chusri
Pharmaceuticals 2023, 16(4), 477; https://doi.org/10.3390/ph16040477 - 23 Mar 2023
Cited by 3 | Viewed by 2216
Abstract
Biofilm-mediated infections are critical to public health and a leading cause of resistance among pathogens, amounting to a prolonged hospital stay and increased mortality rate in the intensive care unit. In this study, the antibacterial and antibiofilm activities of rifampicin or carbapenem monotherapies [...] Read more.
Biofilm-mediated infections are critical to public health and a leading cause of resistance among pathogens, amounting to a prolonged hospital stay and increased mortality rate in the intensive care unit. In this study, the antibacterial and antibiofilm activities of rifampicin or carbapenem monotherapies were compared with rifampicin and carbapenem combination therapies against rifampicin-resistant and carbapenem-resistant Acinetobacter baumannii isolates. Among 29 CRAB isolates, 24/29 (83%) were resistant to rifampicin, with MIC values between 2–256 µg/mL. Checkerboard assays disclosed that combination therapies at FICIs between 1/8 and 1/4 improved the activity of carbapenems at subinhibitory concentrations. Time-kill kinetics indicated a 2- to 4-log reduction at 1/2 MIC rifampicin + 1/4 MIC carbapenem and 1/4 MIC rifampicin + 1/4 MIC carbapenem against the isolates, with the MIC values ranging from 2–8 µg/mL. The MTT assay revealed a dose-dependent decrease of the cell viability of established bacterial biofilm at 4 MIC rifampicin + 2 MIC carbapenems, with a percentage reduction of 44–75%, compared with monotherapies at 16 MIC. Scanning electron microscopy further confirmed bacterial cell membrane disruption, suggesting a synergism between carbapenem and rifampicin against a representative isolate. The findings demonstrated that the combination of rifampicin with carbapenems could improve antibacterial activities and eradicate established Acinetobacter baumannii biofilm. Full article
(This article belongs to the Special Issue Small Molecules as Antimicrobials 2022)
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Review

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39 pages, 7143 KiB  
Review
Transmission-Blocking Strategies for Malaria Eradication: Recent Advances in Small-Molecule Drug Development
by Federico Appetecchia, Emanuele Fabbrizi, Francesco Fiorentino, Sara Consalvi, Mariangela Biava, Giovanna Poce and Dante Rotili
Pharmaceuticals 2024, 17(7), 962; https://doi.org/10.3390/ph17070962 - 19 Jul 2024
Viewed by 1429
Abstract
Malaria drug research and development efforts have resurged in the last decade following the decelerating rate of mortality and malaria cases in endemic regions. The inefficiency of malaria interventions is largely driven by the spreading resistance of the Plasmodium falciparum parasite to current [...] Read more.
Malaria drug research and development efforts have resurged in the last decade following the decelerating rate of mortality and malaria cases in endemic regions. The inefficiency of malaria interventions is largely driven by the spreading resistance of the Plasmodium falciparum parasite to current drug regimens and that of the malaria vector, the Anopheles mosquito, to insecticides. In response to the new eradication agenda, drugs that act by breaking the malaria transmission cycle (transmission-blocking drugs), which has been recognized as an important and additional target for intervention, are being developed. These drugs take advantage of the susceptibility of Plasmodium during population bottlenecks before transmission (gametocytes) and in the mosquito vector (gametes, zygotes, ookinetes, oocysts, sporozoites). To date, compounds targeting stage V gametocytes predominate in the chemical library of transmission-blocking drugs, and some of them have entered clinical trials. The targeting of Plasmodium mosquito stages has recently renewed interest in the development of innovative malaria control tools, which hold promise for the application of compounds effective at these stages. In this review, we highlight the major achievements and provide an update on the research of transmission-blocking drugs, with a particular focus on their chemical scaffolds, antiplasmodial activity, and transmission-blocking potential. Full article
(This article belongs to the Special Issue Small Molecules as Antimicrobials 2022)
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56 pages, 9845 KiB  
Review
Phytochemicals as Antimicrobials: Prospecting Himalayan Medicinal Plants as Source of Alternate Medicine to Combat Antimicrobial Resistance
by Mohammad Vikas Ashraf, Shreekar Pant, M. A. Hannan Khan, Ali Asghar Shah, Sazada Siddiqui, Mouna Jeridi, Heba Waheeb Saeed Alhamdi and Shoeb Ahmad
Pharmaceuticals 2023, 16(6), 881; https://doi.org/10.3390/ph16060881 - 15 Jun 2023
Cited by 19 | Viewed by 7347
Abstract
Among all available antimicrobials, antibiotics hold a prime position in the treatment of infectious diseases. However, the emergence of antimicrobial resistance (AMR) has posed a serious threat to the effectiveness of antibiotics, resulting in increased morbidity, mortality, and escalation in healthcare costs causing [...] Read more.
Among all available antimicrobials, antibiotics hold a prime position in the treatment of infectious diseases. However, the emergence of antimicrobial resistance (AMR) has posed a serious threat to the effectiveness of antibiotics, resulting in increased morbidity, mortality, and escalation in healthcare costs causing a global health crisis. The overuse and misuse of antibiotics in global healthcare setups have accelerated the development and spread of AMR, leading to the emergence of multidrug-resistant (MDR) pathogens, which further limits treatment options. This creates a critical need to explore alternative approaches to combat bacterial infections. Phytochemicals have gained attention as a potential source of alternative medicine to address the challenge of AMR. Phytochemicals are structurally and functionally diverse and have multitarget antimicrobial effects, disrupting essential cellular activities. Given the promising results of plant-based antimicrobials, coupled with the slow discovery of novel antibiotics, it has become highly imperative to explore the vast repository of phytocompounds to overcome the looming catastrophe of AMR. This review summarizes the emergence of AMR towards existing antibiotics and potent phytochemicals having antimicrobial activities, along with a comprehensive overview of 123 Himalayan medicinal plants reported to possess antimicrobial phytocompounds, thus compiling the existing information that will help researchers in the exploration of phytochemicals to combat AMR. Full article
(This article belongs to the Special Issue Small Molecules as Antimicrobials 2022)
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