Next-Generation Antinfective Agents

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

Deadline for manuscript submissions: 31 July 2025 | Viewed by 551

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Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via L. Mangiagalli 25, 20133 Milano, Italy
Interests: protein–protein interaction inhibitors; enzyme inhibitors; multi-target drugs; anticancer agents
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Special Issue Information

Dear Colleagues,

Infectious diseases continue to account for a significant number of deaths worldwide. The rise of antimicrobial resistance is an alarming threat to both human and animal health, driving the search for novel classes of antibiotics to replenish our arsenal against bacterial infections. Furthermore, the profound impact of viral infections and associated pathologies on global health in recent years has prompted scientists to address the challenges and opportunities related to the development of effective antiviral agents with new mechanisms of action. The discovery of new antimicrobials/antivirals, as well as the repurposing of existing drugs, will be crucial in combating the growing resistance of "superbugs", pathogenic fungi, viruses, and parasites.

In this Special Issue, Pharmaceuticals welcomes the submission of both review articles and original research papers that highlight recent advances in medicinal chemistry, with a particular focus on novel antibacterial and antiviral agents. The scope of this Special Issue includes, but is not limited to, natural product screening, the identification and validation of novel antibacterial/antiviral targets, and strategies for the discovery and optimization of new compounds.

Dr. Fiorella Meneghetti
Prof. Dr. Daniela Barlocco
Guest Editors

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Keywords

  • small molecules
  • peptides
  • peptidomimetics
  • bacterial infections
  • fungi
  • virus
  • parasites
  • drug design
  • computational tools
  • biology assays
  • resistance mechanisms

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Published Papers (1 paper)

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Research

36 pages, 2017 KiB  
Article
Anti-Infective Properties, Cytotoxicity, and In Silico ADME Parameters of Novel 4′-(Piperazin-1-yl)benzanilides
by Theresa Hermann, Sarah Harzl, Robin Wallner, Elke Prettner, Eva-Maria Pferschy-Wenzig, Monica Cal, Pascal Mäser and Robert Weis
Pharmaceuticals 2025, 18(7), 1004; https://doi.org/10.3390/ph18071004 - 3 Jul 2025
Viewed by 366
Abstract
Background: The benzamide MMV030666 from MMV’s Malaria Box Project, the starting point of herein presented study, was initially tested against various Plasmodium falciparum strains as well as Gram-positive and Gram-negative bacteria. It exhibits multi-stage antiplasmodial potencies and lacks resistance development. Methods: [...] Read more.
Background: The benzamide MMV030666 from MMV’s Malaria Box Project, the starting point of herein presented study, was initially tested against various Plasmodium falciparum strains as well as Gram-positive and Gram-negative bacteria. It exhibits multi-stage antiplasmodial potencies and lacks resistance development. Methods: The favorable structural features from previous series were kept while the influence of the N-Boc-piperazinyl substituent per se, as well as its ring position and its replacement by various heteroaromatic rings, was evaluated. Thus, this paper describes the preparation of the MMV030666-derived 4′-(piperazin-1-yl)benzanilides for the first time, exhibiting broad-spectrum activity not only against plasmodia but also various bacterial strains. Results: A series of insightful structure–activity relationships were determined. Furthermore, pharmacokinetic and physicochemical parameters of the new compounds were determined experimentally or in silico. Drug-likeliness according to Lipinski’s rules was calculated as well. Conclusions: A diarylthioether derivative of the lead compound was promisingly active against P. falciparum and exhibited broad-spectrum antibacterial activity against Gram-positive as well as Gram-negative bacteria. It is considered for testing against multi-resistant bacterial strains and in vivo studies. Full article
(This article belongs to the Special Issue Next-Generation Antinfective Agents)
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