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Tuberculosis Drug Discovery and Development

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

Deadline for manuscript submissions: closed (30 September 2019) | Viewed by 7561

Special Issue Editors


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Guest Editor
Universita degli Studi di Modena e Reggio Emilia, Dipartimento di Scienze della Vita, Modena, Italy
Interests: medicinal chemistry; synthesis; drug delivery; neglected diseases

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Co-Guest Editor
Department of Pharmaceutical Sciences, University of Milan, Via L. Mangiagalli 25, 20133 Milano, Italy
Interests: diffraction techniques; structure elucidation; conformation of bioactive compounds; antitubercular and anticancer agents; metal complexes, protein–protein interaction inhibitors; enzymatic inhibitors; multi-target drugs
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Special Issue Information

Dear Colleagues,

We are pleased to announce that submissions for the Molecules Special Issue “Tuberculosis in Drug Discovery and Development” are now open.

According to the World Health Organization, tuberculosis, caused by Mycobacterium tuberculosis, is an infectious disease that causes the highest number of deaths worldwide. Standard treatments with antibiotics are long and complex, and drug resistance is growing rapidly: even for recently approved bedaquiline, delamanid, and linezolid, resistance has already emerged. Thus, there is a great unmet medical need and, consequently, a great interest in the opportunities and challenges associated with tackling tuberculosis, in order to develop effective and, possibly, cheap antimycobacterial agents endowed with new mechanisms of action.

This issue will cover multiple aspects of the search for new molecules starting both from natural and synthetic compounds and addressing different or multiple targets (multitarget drugs) in Mycobacterium tuberculosis. Original research articles, as well as reviews, that are able to make substantial advances in this field are welcome.

Prof. Dr. Luca Costantino
Prof. Dr. Fiorella Meneghetti
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. 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

  • Small molecules
  • Peptides
  • Peptidomimetics
  • Mycobacterial target
  • Drug design
  • Computational tools
  • Resistance mechanisms
  • Crystallography
  • Structure-property relationships
  • Bioavailability
  • Pharmacokinetics

Published Papers (2 papers)

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Research

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14 pages, 8559 KiB  
Article
Discovery of (3-Benzyl-5-hydroxyphenyl)carbamates as New Antitubercular Agents with Potent In Vitro and In Vivo Efficacy
by Ya-Juan Cheng, Zhi-Yong Liu, Hua-Ju Liang, Cui-Ting Fang, Niu-Niu Zhang, Tian-Yu Zhang and Ming Yan
Molecules 2019, 24(10), 2021; https://doi.org/10.3390/molecules24102021 - 27 May 2019
Cited by 5 | Viewed by 3409
Abstract
A series of 3-amino-5-benzylphenol derivatives were designed and synthesized. Among them, (3-benzyl-5-hydroxyphenyl)carbamates were found to exert good inhibitory activity against M. tuberculosis H37Ra, H37Rv and clinically isolated multidrug-resistant M. tuberculosis strains (MIC = 0.625–6.25 μg/mL). The privileged compounds 3i and 3l showed moderate [...] Read more.
A series of 3-amino-5-benzylphenol derivatives were designed and synthesized. Among them, (3-benzyl-5-hydroxyphenyl)carbamates were found to exert good inhibitory activity against M. tuberculosis H37Ra, H37Rv and clinically isolated multidrug-resistant M. tuberculosis strains (MIC = 0.625–6.25 μg/mL). The privileged compounds 3i and 3l showed moderate cytotoxicity against cell line A549. Compound 3l also exhibited potent in vivo inhibitory activity on a mouse infection model via the oral administration. The results demonstrated 3-hydroxyphenylcarbamates as a class of new antitubercular agents with good potential. Full article
(This article belongs to the Special Issue Tuberculosis Drug Discovery and Development)
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Review

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16 pages, 271 KiB  
Review
Phenolic Compounds as Promising Drug Candidates in Tuberculosis Therapy
by Muhamad Harith Mazlun, Siti Fatimah Sabran, Maryati Mohamed, Mohd Fadzelly Abu Bakar and Zunoliza Abdullah
Molecules 2019, 24(13), 2449; https://doi.org/10.3390/molecules24132449 - 04 Jul 2019
Cited by 20 | Viewed by 3781
Abstract
Tuberculosis (TB), caused by Mycobacterium tuberculosis (MTB) remains one of the deadliest, infectious diseases worldwide. The detrimental effects caused by the existing anti-TB drugs to TB patients and the emergence of resistance strains of M. tuberculosis has driven efforts from natural products researchers [...] Read more.
Tuberculosis (TB), caused by Mycobacterium tuberculosis (MTB) remains one of the deadliest, infectious diseases worldwide. The detrimental effects caused by the existing anti-TB drugs to TB patients and the emergence of resistance strains of M. tuberculosis has driven efforts from natural products researchers around the globe in discovering novel anti-TB drugs that are more efficacious and with less side effects. There were eleven main review publications that focused on natural products with anti-TB potentials. However, none of them specifically emphasized antimycobacterial phenolic compounds. Thus, the current review’s main objective is to highlight and summarize phenolic compounds found active against mycobacteria from 2000 to 2017. Based on the past studies in the electronic databases, the present review also focuses on several test organisms used in TB researches and their different distinct properties, a few types of in vitro TB bioassay and comparison between their strengths and drawbacks, different methods of extraction, fractionation and isolation, ways of characterizing and identifying isolated compounds and the mechanism of actions of anti-TB phenolic compounds as reported in the literature. Full article
(This article belongs to the Special Issue Tuberculosis Drug Discovery and Development)
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