ijms-logo

Journal Browser

Journal Browser

Special Issue "New Molecular Designs for Drugs including Potential Antibiotics"

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Biochemistry".

Deadline for manuscript submissions: closed (31 July 2022) | Viewed by 1237

Special Issue Editors

Prof. Dr. David StC Black
E-Mail Website
Guest Editor
School of Chemistry, University of New South Wales (UNSW Sydney), Sydney, NSW 2052, Australia
Interests: heterocyclic chemistry; synthetic organic chemistry; natural products chemistry; new indole-based scaffolds; synthetic methodologies
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Naresh Kumar
E-Mail Website
Guest Editor
School of Chemistry, University of New South Wales, UNSW Sydney, Sydney, NSW 2052, Australia
Interests: biologically active molecules; medicinal chemistry; organic chemical synthesis; peptidomimetics; novel antimicrobials; biomaterials
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Living systems are the source of a diverse range of bioactive chemicals in many different ways. Naturally produced chemicals are of fundamental importance in biological systems and are used to mediate interactions across all levels of biological hierarchy. Natural products have also been the inspiration for semi-synthetic modifications, or as lead platforms for the synthesis of functional analogues targeted against specific receptors. Synthetic methodology allows the design and synthesis of completely new, yet active, “unnatural” structural types. Utilizing modern synthetic organic chemistry and “natural leads”, novel biologically active molecules can be developed for biological properties, including antimicrobial, anti-inflammatory and anticancer properties.

This Special Issue aims to cover a diverse range of synthetic and natural biologically active molecules for potential leads for drug discovery. Contributions from synthetic chemists, medicinal chemists, molecular biologists and pharmacologists are sought for this multi-disciplinary issue. In addition to manuscripts on the latest results, reviews are also encouraged.

Prof. Dr. David StC Black
Prof. Dr. Naresh Kumar
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 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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. 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

  • design and synthesis of novel biologically active molecules
  • new targets for antibiotic discovery
  • structure based drug design
  • novel scaffolds for drug discovery
  • peptide mimics
  • cell-to-cell communication (e.g., quorum sensing)

Published Papers (1 paper)

Order results
Result details
Select all
Export citation of selected articles as:

Research

Article
Cholic Acid-Based Antimicrobial Peptide Mimics as Antibacterial Agents
Int. J. Mol. Sci. 2022, 23(9), 4623; https://doi.org/10.3390/ijms23094623 - 21 Apr 2022
Cited by 1 | Viewed by 667
Abstract
There is a significant and urgent need for the development of novel antibacterial agents to tackle the increasing incidence of antibiotic resistance. Cholic acid-based small molecular antimicrobial peptide mimics are reported as potential new leads to treat bacterial infection. Here, we describe the [...] Read more.
There is a significant and urgent need for the development of novel antibacterial agents to tackle the increasing incidence of antibiotic resistance. Cholic acid-based small molecular antimicrobial peptide mimics are reported as potential new leads to treat bacterial infection. Here, we describe the design, synthesis and biological evaluation of cholic acid-based small molecular antimicrobial peptide mimics. The synthesis of cholic acid analogues involves the attachment of a hydrophobic moiety at the carboxyl terminal of the cholic acid scaffold, followed by the installation of one to three amino acid residues on the hydroxyl groups present on the cholic acid scaffold. Structure–activity relationship studies suggest that the tryptophan moiety is important for high antibacterial activity. Moreover, a minimum of +2 charge is also important for antimicrobial activity. In particular, analogues containing lysine-like residues showed the highest antibacterial potency against Gram-positive S. aureus. All di-substituted analogues possess high antimicrobial activity against both Gram-positive S. aureus as well as Gram-negative E. coli and P. aeruginosa. Analogues 17c and 17d with a combination of these features were found to be the most potent in this study. These compounds were able to depolarise the bacterial membrane, suggesting that they are potential antimicrobial pore forming agents. Full article
(This article belongs to the Special Issue New Molecular Designs for Drugs including Potential Antibiotics)
Show Figures

Figure 1

Back to TopTop