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Antibiotics
Special Issues
Evaluation of Emerging Antimicrobials
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Evaluation of Emerging Antimicrobials

A special issue of Antibiotics (ISSN 2079-6382).

Deadline for manuscript submissions: 31 May 2025 | Viewed by 4044

Special Issue Editor

Dr. Dilep Kumar Sigalapalli

E-Mail Website
Guest Editor
Department of Biochemistry, University of Washington, Seattle, WA, USA
Interests: drug design and synthesis; chemistry; cancer; infectious diseases; pharmacology

Special Issue Information

Dear Colleagues,

Antimicrobials are therapeutic agents used in the treatment and/or prevention of infections. They include antibiotics, antivirals, antifungals, antiparasitics, and antiseptics. Antimicrobial agents can interfere with cellular processes like cell wall/membrane synthesis and the activity of cellular enzymes, thereby preventing their growth, or they can directly kill the microorganisms. As defined by the WHO (World Health Organization), antimicrobial resistance occurs when microorganisms change over time and do not respond to treatment, thereby making infections difficult to treat and increasing their severity and spread, leading to death. The overuse and misuse of antimicrobials is a serious driver of antimicrobial resistance. Antimicrobial resistance is a global concern and demands the urgent development of novel antimicrobial agents with diverse chemical structures and novel mechanisms of action to overcome it.

This Special Issue aims to present new chemical agents (NCEs) and their antimicrobial evaluation against different microorganisms. It also encourages any novel advances in the mechanistic insights of known antimicrobial agents toward infections.

We look forward to receiving your contributions.

Dr. Dilep Kumar Sigalapalli
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. Antibiotics 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

  • antibacterials
  • antibiotics
  • antifungals
  • antimicrobial agents
  • antimicrobial resistance
  • antivirals
  • bacterial resistance
  • infections
  • multidrug resistance
  • pathogens

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Further information on MDPI's Special Issue polices can be found here.

Published Papers (2 papers)

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Research

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17 pages, 3306 KiB  
Article
Naturally Derived Malabaricone B as a Promising Bactericidal Candidate Targeting Multidrug-Resistant Staphylococcus aureus also Possess Synergistic Interactions with Clinical Antibiotics
by Neethu Sivadas, Grace Kaul, Abdul Akhir, Manjulika Shukla, Murugan Govindakurup Govind, Mathew Dan, Kokkuvayil Vasu Radhakrishnan and Sidharth Chopra
Antibiotics 2023, 12(10), 1483; https://doi.org/10.3390/antibiotics12101483 - 26 Sep 2023
Cited by 3 | Viewed by 1702
Abstract
The emergence of multidrug-resistant (MDR) superbugs underlines the urgent need for innovative treatment options to tackle resistant bacterial infections. The clinical efficacy of natural products directed our efforts towards developing new antibacterial leads from naturally abundant known chemical structures. The present study aimed [...] Read more.
The emergence of multidrug-resistant (MDR) superbugs underlines the urgent need for innovative treatment options to tackle resistant bacterial infections. The clinical efficacy of natural products directed our efforts towards developing new antibacterial leads from naturally abundant known chemical structures. The present study aimed to explore an unusual class of phenylacylphenols (malabaricones) from Myristicamalabarica as antibacterial agents. In vitro antibacterial activity was determined via broth microdilution, cell viability, time–kill kinetics, biofilm eradication, intracellular killing, and checkerboard assays. The efficacy was evaluated in vivo in murine neutropenic thigh and skin infection models. Confocal and SEM analyses were used for mechanistic studies. Among the tested isolates, malabaricone B (NS-7) demonstrated the best activity against S. aureus with a favorable selectivity index and concentration-dependent, rapid bactericidal killing kinetics. It displayed equal efficacy against MDR clinical isolates of S. aureus and Enterococci, efficiently clearing S. aureus in intracellular and biofilm tests, with no detectable resistance. In addition, NS-7 synergized with daptomycin and gentamicin. In vivo, NS-7 exhibited significant efficacy against S. aureus infection. Mechanistically, NS-7 damaged S. aureus membrane integrity, resulting in the release of extracellular ATP. The results indicated that NS-7 can act as a naturally derived bactericidal drug lead for anti-staphylococcal therapy. Full article
(This article belongs to the Special Issue Evaluation of Emerging Antimicrobials)
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Review

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18 pages, 3584 KiB  
Review
Bacterial Histidine Kinase and the Development of Its Inhibitors in the 21st Century
by Ragib Ahsan, Sumaiya Kifayat, Krishan Kumar Pooniya, Sunita Kularia, Bhavani Sailu Adimalla, Bharat Kumar Reddy Sanapalli, Vidyasrilekha Sanapalli and Dilep Kumar Sigalapalli
Antibiotics 2024, 13(7), 576; https://doi.org/10.3390/antibiotics13070576 - 22 Jun 2024
Viewed by 1542
Abstract
Bacterial histidine kinase (BHK) is a constituent of the two-component signaling (TCS) pathway, which is responsible for the regulation of a number of processes connected to bacterial pathogenicity, virulence, biofilm development, antibiotic resistance, and bacterial persistence. As BHK regulation is diverse, inhibitors can [...] Read more.
Bacterial histidine kinase (BHK) is a constituent of the two-component signaling (TCS) pathway, which is responsible for the regulation of a number of processes connected to bacterial pathogenicity, virulence, biofilm development, antibiotic resistance, and bacterial persistence. As BHK regulation is diverse, inhibitors can be developed, such as antibiotic synergists, bacteriostatic/bactericidal agents, virulence inhibitors, and biofilm inhibitors. Inhibition of essential BHK has always been an amenable strategy due to the conserved binding sites of the domains across bacterial species and growth dependence. Hence, an inhibitor of BHK might block multiple TCS regulatory networks. This review describes the TCS system and the role of BHK in bacterial virulence and discusses the available inhibitors of BHK, which is a specific response regulator with essential structural features. Full article
(This article belongs to the Special Issue Evaluation of Emerging Antimicrobials)
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