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Molecules
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New Potential Antimicrobial Agents: Design, Synthesis and Biological Evaluation
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New Potential Antimicrobial Agents: Design, Synthesis and Biological Evaluation

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (30 September 2023) | Viewed by 3488

Special Issue Editor

Dr. Vijai Kumar Reddy Tangadanchu

E-Mail Website1 Website2
Guest Editor
Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA
Interests: drug design; medicinal chemistry; organic synthesis, radiopharmaceuticals; antifungal; antibacterial; DNA targeting potentiators; membrane-active drugs

Special Issue Information

Dear Colleagues,

Antimicrobial resistance is one of the greatest challenges facing the world today. The serendipitous discovery of penicillin in 1928 forever changed the medical landscape and paved the way for future pharmacological breakthroughs. However, since the 1960s, the number of multi-drug resistant bacteria has continued to increase, and only a small number of novel classes of antibiotics have entered the market. According to the Centers of Disease Control and Prevention (CDC), 23,000 individuals die annually in the United States (US) alone as a result of antibiotic-resistant infections. Further, recently the World Health Organization (WHO) titled a recent world health day “Combat drug resistance: no action today means no cure tomorrow”. Hence, given the increasing prevalence of antibiotic-resistant pathogens and a paucity of novel therapeutics capable of withstanding antibiotic-induced selective pressure, a great deal of research is being carried out to identify and develop new structural classes of effective antimicrobials to help combat the current global health threat. This includes searching for potentiators of the activity of known antimicrobial agents and the development of hybrid molecules, novel membrane-active drugs, and inhibitors of bacterial virulence and pathogenesis. All these make the fight against microbial infections a challenging global issue and underscore the urgent need to develop potent and appropriate antimicrobials.

Dr. Vijai Kumar Reddy Tangadanchu
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. Molecules is an international peer-reviewed open access semimonthly 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 2700 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

  • drug design
  • structure activity relationship
  • multi-drug resistance
  • antifungal
  • antibacterial
  • DNA targeting antimicrobial agents
  • membrane-active drugs
  • molecular modeling

Published Papers (2 papers)

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Research

11 pages, 910 KiB  
Article
Development of Novel Isatin-Tethered Quinolines as Anti-Tubercular Agents against Multi and Extensively Drug-Resistant Mycobacterium tuberculosis
by Mohamed A. Abdelrahman, Hadia Almahli, Tarfah Al-Warhi, Taghreed A. Majrashi, Marwa M. Abdel-Aziz, Wagdy M. Eldehna and Mohamed A. Said
Molecules 2022, 27(24), 8807; https://doi.org/10.3390/molecules27248807 - 12 Dec 2022
Cited by 11 | Viewed by 1423
Abstract
We describe the design and synthesis of two isatin-tethered quinolines series (Q6a–h and Q8a–h), in connection with our research interest in developing novel isatin-bearing anti-tubercular candidates. In a previous study, a series of small molecules bearing a [...] Read more.
We describe the design and synthesis of two isatin-tethered quinolines series (Q6a–h and Q8a–h), in connection with our research interest in developing novel isatin-bearing anti-tubercular candidates. In a previous study, a series of small molecules bearing a quinoline-3-carbohydrazone moiety was developed as anti-tubercular agents, and compound IV disclosed the highest potency with MIC value equal to 6.24 µg/mL. In the current work, we adopted the bioisosteric replacement approach to replace the 3,4,5-trimethoxy-benzylidene moiety in the lead compound IV with the isatin motif, a privileged scaffold in the TB drug discovery, to furnish the first series of target molecules Q6a–h. Thereafter, the isatin motif was N-substituted with either a methyl or benzyl group to furnish the second series Q8a–h. All of the designed quinoilne-isatin conjugates Q6a–h and Q8a–h were synthesized and then biologically assessed for anti-tubercular actions towards drug-susceptible, MDR, and XDR strains. Superiorly, the N-benzyl-bearing compound Q8b possessed the best activities against the examined M. tuberculosis strains with MICs equal 0.06, 0.24, and 1.95 µg/mL, respectively. Full article
(This article belongs to the Special Issue New Potential Antimicrobial Agents: Design, Synthesis and Biological Evaluation)
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22 pages, 3580 KiB  
Article
Identification of Novel Antifungal Skeleton of Hydroxyethyl Naphthalimides with Synergistic Potential for Chemical and Dynamic Treatments
by Pengli Zhang, Vijai Kumar Reddy Tangadanchu and Chenghe Zhou
Molecules 2022, 27(23), 8453; https://doi.org/10.3390/molecules27238453 - 02 Dec 2022
Cited by 9 | Viewed by 1195
Abstract
The invasion of pathogenic fungi poses nonnegligible threats to the human health and agricultural industry. This work exploited a family of hydroxyethyl naphthalimides as novel antifungal species with synergistic potential of chemical and dynamic treatment to combat the fungal resistance. These prepared naphthalimides [...] Read more.
The invasion of pathogenic fungi poses nonnegligible threats to the human health and agricultural industry. This work exploited a family of hydroxyethyl naphthalimides as novel antifungal species with synergistic potential of chemical and dynamic treatment to combat the fungal resistance. These prepared naphthalimides showed better antifungal potency than fluconazole towards some tested fungi including Aspergillus fumigatus, Candida tropicalis and Candida parapsilosis 22019. Especially, thioether benzimidazole derivative 7f with excellent anti-Candida tropicalis efficacy (MIC = 4 μg/mL) possessed low cytotoxicity, safe hemolysis level and less susceptibility to induce resistance. Biochemical interactions displayed that 7f could form a supramolecular complex with DNA to block DNA replication, and constitute a biosupermolecule with cytochrome P450 reductase (CPR) from Candida tropicalis to hinder CPR biological function. Additionally, 7f presented strong lipase affinity, which facilitated its permeation into cell membrane. Moreover, 7f with dynamic antifungal potency promoted the production and accumulation of reactive oxygen species (ROS) in cells, which destroyed the antioxidant defence system, led to oxidative stress with lipid peroxidation, loss of glutathione, membrane dysfunction and metabolic inactivation, and eventually caused cell death. The chemical and dynamic antifungal synergistic effect initiated by hydroxyethyl naphthalimides was a reasonable treatment window for prospective development. Full article
(This article belongs to the Special Issue New Potential Antimicrobial Agents: Design, Synthesis and Biological Evaluation)
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