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Chirality in Drugs and Drug Candidates
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Chirality in Drugs and Drug Candidates

A topical collection in Drugs and Drug Candidates (ISSN 2813-2998). This collection belongs to the section "Medicinal Chemistry and Preliminary Screening".

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Editors

Dr. Carla Fernandes

E-Mail Website
Collection Editor
1. Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal
2. Centro Interdisciplinar de Investigação Marinha e Ambiental (CIIMAR/CIMAR), Universidade do Porto, Edifício do Terminal de Cruzeiros do Porto de Leixões, Av. General Norton de Matos s/n, 4050-208 Matosinhos, Portugal
Interests: medicinal chemistry; organic chemistry; chiral bioactive substances; enantioselective studies; chirality; chromatography
Special Issues, Collections and Topics in MDPI journals
Dr. Maria Emília De Sousa

E-Mail Website1 Website2
Collection Editor
1. Interdisciplinary Centre of Marine and Environmental Research (CIIMAR), 4450-208 Porto, Portugal
2. Laboratory of Organic and Pharmaceutical Chemistry, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
Interests: medicinal chemistry; organic synthesis; heterocycles; P-glycoprotein; anticancer; antimicrobials; chiral drugs; marine natural products
Special Issues, Collections and Topics in MDPI journals

Topical Collection Information

Dear Colleagues,

Over the last several years, the relationship between chirality and therapeutic activities has been of increasing importance in the drug discovery pipeline. Chirality is ubiquitous in biological systems, and can therefore have a key influence on drug pharmacodynamics, pharmacokinetics, and toxicity. Chirality can now be considered one of the major topics in the design, discovery, synthesis, development, evaluation, and marketing of new drugs, both for human and veterinary use. In addition to the increase of chiral drugs in the market, the relevance of enantioselective studies boosts each year due to advantages in potency, efficacy, selectivity, and safety associated with the use of single enantiomers. The advances in enantioselective synthesis as well as enantioseparation methodologies aligned to the stricter requirements from regulatory authorities to patent new chiral drugs led to increased research in this field.

This Topical Collection invites critical reviews, original research articles and other formats with comprehensive theoretical and experimental details focused on all aspects of chirality involved in drugs and drug candidates. This Topical Collection has the broad goal of illustrating recent and future trends in the development of successful chiral drugs and the search for new promising chiral drug candidates. Topics include the discovery, design and development of new chiral leads as well as synthetic and natural chiral drugs; chiral recognition studies; enantioselective synthesis; enantiomeric resolution; chiral drug analysis; stereochemical elucidation; and enantioselective studies on drug and drug candidate pharmacodynamics, pharmacokinetics, toxicity, and environment.

Dr. Maria Emília De Sousa
Dr. Carla Fernandes
Collection 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 collection 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. Drugs and Drug Candidates is an international peer-reviewed open access quarterly 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 1000 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

  • synthetic and natural chiral drugs
  • novel chiral drug candidates
  • chiral recognition
  • enantioselective synthesis
  • enantioresolution
  • chiral analysis
  • enantioselective studies

Published Papers (2 papers)

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2024

20 pages, 4230 KiB  
Review
Chirality in Modern Antidepressants: A Comprehensive Review of Stereochemical Impacts on Pharmacology and Therapeutics
by Gabriel Hancu, Alexandra Uilăcan and Nicoleta Mirela Blebea
Drugs Drug Candidates 2024, 3(4), 654-673; https://doi.org/10.3390/ddc3040037 - 27 Sep 2024
Viewed by 1046
Abstract
The review explores the critical role of chirality in the pharmacology of antidepressant drugs, focusing on how the stereochemistry of these compounds influences their biological activity and therapeutic outcomes. Antidepressants, especially modern classes such as selective serotonin reuptake inhibitors (SSRIs) and serotonin–norepinephrine reuptake [...] Read more.
The review explores the critical role of chirality in the pharmacology of antidepressant drugs, focusing on how the stereochemistry of these compounds influences their biological activity and therapeutic outcomes. Antidepressants, especially modern classes such as selective serotonin reuptake inhibitors (SSRIs) and serotonin–norepinephrine reuptake inhibitors (SNRIs), often possess chiral centers that result in enantiomers with distinct pharmacodynamic and pharmacokinetic profiles. The review systematically examines various chiral antidepressants, including racemic mixtures and enantiomerically pure drugs, highlighting the differential effects of each enantiomer on neurotransmitter reuptake inhibition and the potential clinical implications. By examining specific examples of chiral antidepressants, the review illustrates the differences in pharmacokinetics and pharmacodynamics between enantiomers and racemic mixtures, emphasizing the clinical advantages of using enantiomerically pure compounds. Understanding and leveraging chirality in drug design and therapy is crucial for optimizing antidepressant treatments, offering insights into future research directions that could enhance patient outcomes by tailoring medication more precisely to individual biological profiles. Full article
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13 pages, 4237 KiB  
Article
Design of Marine Cyclodepsipeptide Analogues Targeting Candida albicans Efflux Pump CaCdr1p
by Ricardo Ribeiro, Sara Fortes, Lia Costa, Andreia Palmeira, Eugénia Pinto, Emília Sousa and Carla Fernandes
Drugs Drug Candidates 2024, 3(3), 537-549; https://doi.org/10.3390/ddc3030031 - 1 Aug 2024
Viewed by 934
Abstract
Fungal infections are a significant threat to human health and the environment. The emergence of multidrug-resistant strains of fungi and the growing prevalence of azole resistance in invasive fungal infections exacerbate the problem, with efflux pumps being a major cause of antifungal resistance [...] Read more.
Fungal infections are a significant threat to human health and the environment. The emergence of multidrug-resistant strains of fungi and the growing prevalence of azole resistance in invasive fungal infections exacerbate the problem, with efflux pumps being a major cause of antifungal resistance and a prime target for several counteractive strategies. In Candida albicans, the ATP-binding cassette superfamily transporter CaCdr1p is the predominant efflux pump involved in azole resistance. Marine organisms have unique phenotypic characteristics to survive in challenging environments, resulting in biologically active compounds. The cyclodepsipeptides unnarmicin A and C have shown promising results as inhibitors of rhodamine 6G efflux in cells expressing CaCdr1p. Herein, a series of unnarmicin analogues were designed and docked against a CaCdr1p efflux pump based on the cryogenic electron microscopy structure available to select the most promising compounds. Analogue 33 was predicted to be the best considering its high affinity for the efflux pump and pharmacokinetic profile. These results pave the way for further synthesis and in vitro biological studies of novel unnarmicins seeking a synergistic effect with fluconazole. Full article
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