Discovery and Development of New Antimycobacterial Agents

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

Deadline for manuscript submissions: closed (15 March 2024) | Viewed by 1521

Special Issue Editors


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Guest Editor
InSiliTox, Department of Pharmacy, Faculty of Health Sciences, University of Brasilia, Brasilia 70910-900, Brazil
Interests: drug discovery; tuberculosis; molecular dynamics; therapeutic drugs toxicology

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Guest Editor
Natural Products Laboratory, Department of Pharmacy, Health Sciences School, University of Brasilia, Brasilia 70910-900, Brazil
Interests: enzymology; bioprocess; biotechnology

Special Issue Information

Dear Colleagues,

We would like to invite you to submit your research papers on drug development for tuberculosis (TB) treatment to the Pharmaceuticals Special Issue "Discovery and Development of New Antimycobacterial Agents". TB continues to be a major global health challenge, and it is essential to put together the latest advancements in drug development to address this critical issue. Your contribution to this field is valuable, and we believe that a manuscript of your work can impact the fight against TB.

The papers should cover the current state-of-the-art in drug development for tuberculosis, including innovative approaches to the discovery, development, and delivery of new treatments. The scope of the papers can also include in silico, in vitro, preclinical and clinical studies, pharmacokinetics, pharmacodynamics, and toxicity.

Potential topics to be covered include, but are not limited to:

  • Chemical development of novel and effective antimycobacterial drugs;
  • In silico drug design with at least in vitro results corroborating the computational analysis;
  • Evaluation of natural product derivatives’ efficacy against Mycobacterium;
  • Novel drug repurposing proposals with at least in vitro results;
  • New strategies to avoid or overcome drug resistance;
  • Evaluation of new molecular targets, evidencing their potential effectiveness in therapeutics;
  • Innovative drug delivery systems for TB treatment;
  • Cutting-edge approaches to the development of original and functional antimycobacterial drugs.

Dr. Maurício Homem-De-Mello
Prof. Dr. Pérola de Oliveira Magalhães
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. Pharmaceuticals 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

  • tuberculosis
  • drug discovery
  • drug design
  • drug repurposing
  • TB molecular targets
  • TB drug delivery systems

Published Papers (1 paper)

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Research

19 pages, 2974 KiB  
Article
Novel Derivatives of Quinoxaline-2-carboxylic Acid 1,4-Dioxides as Antimycobacterial Agents: Mechanistic Studies and Therapeutic Potential
by Svetlana G. Frolova, Aleksey A. Vatlin, Dmitry A. Maslov, Buhari Yusuf, Galina I. Buravchenko, Olga B. Bekker, Ksenia M. Klimina, Svetlana V. Smirnova, Lidia M. Shnakhova, Irina K. Malyants, Arseniy I. Lashkin, Xirong Tian, Md Shah Alam, George V. Zatonsky, Tianyu Zhang, Andrey E. Shchekotikhin and Valery N. Danilenko
Pharmaceuticals 2023, 16(11), 1565; https://doi.org/10.3390/ph16111565 - 06 Nov 2023
Cited by 2 | Viewed by 1169
Abstract
The World Health Organization (WHO) reports that tuberculosis (TB) is one of the top 10 leading causes of global mortality. The increasing incidence of multidrug-resistant TB highlights the urgent need for an intensified quest to discover innovative anti-TB medications In this study, we [...] Read more.
The World Health Organization (WHO) reports that tuberculosis (TB) is one of the top 10 leading causes of global mortality. The increasing incidence of multidrug-resistant TB highlights the urgent need for an intensified quest to discover innovative anti-TB medications In this study, we investigated four new derivatives from the quinoxaline-2-carboxylic acid 1,4-dioxide class. New 3-methylquinoxaline 1,4-dioxides with a variation in substituents at positions 2 and 6(7) were synthesized via nucleophilic aromatic substitution with amines and assessed against a Mycobacteria spp. Compound 4 showed high antimycobacterial activity (1.25 μg/mL against M. tuberculosis) and low toxicity in vivo in mice. Selection and whole-genomic sequencing of spontaneous drug-resistant M. smegmatis mutants revealed a high number of single-nucleotide polymorphisms, confirming the predicted mode of action of the quinoxaline-2-carboxylic acid 1,4-dioxide 4 as a DNA-damaging agent. Subsequent reverse genetics methods confirmed that mutations in the genes MSMEG_4646, MSMEG_5122, and MSMEG_1380 mediate resistance to these compounds. Overall, the derivatives of quinoxaline-2-carboxylic acid 1,4-dioxide present a promising scaffold for the development of innovative antimycobacterial drugs. Full article
(This article belongs to the Special Issue Discovery and Development of New Antimycobacterial Agents)
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