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Organic Compounds and Nanoparticles Studies for Applications in Cancer and Tuberculosis Therapeutics

A special issue of Materials (ISSN 1996-1944). This special issue belongs to the section "Biomaterials".

Deadline for manuscript submissions: closed (20 February 2023) | Viewed by 3364

Special Issue Editors

Dr. Katarzyna Gobis

E-Mail Website
Guest Editor
Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Gdańsk, Gdańsk, Poland
Interests: organic synthesis; anti-tuberculosis activity; SAR-analysis; design of active compounds
Dr. Anita Bułakowska

E-Mail Website
Guest Editor
Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Gdańsk, Gdańsk, Poland
Interests: organic synthesis; anti-cancer activity; SAR-analysis; biological evaluation

Special Issue Information

Dear Colleagues,

Cancers are among the leading causes of death worldwide, with 18 million new cases and almost 10 million cancer-related deaths in 2020. They particularly affect the societies of developed countries, where theoretically there is no problem with access to medical care. However, a huge therapeutic problem is the toxicity of clinically used therapeutics and the resistance of cancer cells to the treatment used. Tuberculosis is also very dangerous disease, resulting in large number of patients and deaths. Approximately one third of the world population is infected with Mycobarcterium tuberculosis. Each year about 9 million people become ill and almost 4 million die. The problem concerns not only the poor countries, which cannot afford the long and expensive treatment. The spreading of the disease is observed also in the developed countries due to appearance of the multidrug-resistant (MDR-TB) and extremely drug-resistant (XDR) strains of the bacteria. The situation of sick people was additionally worsened by the SARS-CoV-2 pandemic. The ongoing war in Ukraine and the population movement associated with it will probably also be of importance.

This special edition aims to bring together original works on the design, synthesis and potential of organic compounds and nanoparticles for their use as cancer and tuberculosis therapeutics. We look forward to receiving your submissions for this special issue. Full articles, short announcements and reviews are welcome.

Dr. Katarzyna Gobis
Dr. Anita Bułakowska
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. Materials 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 2600 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

  • organic compounds
  • nanoparticles
  • anti-cancer
  • anti-tuberculosis
  • design
  • synthesis
  • structural activity relationship (SAR)

Published Papers (2 papers)

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Research

19 pages, 3565 KiB  
Article
Synthesis and Structure–Activity Relationship of 2,6-Disubstituted Thiosemicarbazone Derivatives of Pyridine as Potential Antituberculosis Agents
by Dagmara Ziembicka, Katarzyna Gobis, Małgorzata Szczesio, Andrzej Olczak, Ewa Augustynowicz-Kopeć, Agnieszka Głogowska, Izabela Korona-Głowniak and Krzysztof Bojanowski
Materials 2023, 16(1), 448; https://doi.org/10.3390/ma16010448 - 3 Jan 2023
Cited by 5 | Viewed by 1710
Abstract
In this study, six new 2,6-disubstituted thiosemicarbazone derivatives of pyridine were synthesized (4–9), and their tuberculostatic activity was evaluated. All of them showed two- to eightfold higher activity (minimum inhibitory concentration (MIC) 0.5–4 µg/mL) against the resistant strain compared [...] Read more.
In this study, six new 2,6-disubstituted thiosemicarbazone derivatives of pyridine were synthesized (4–9), and their tuberculostatic activity was evaluated. All of them showed two- to eightfold higher activity (minimum inhibitory concentration (MIC) 0.5–4 µg/mL) against the resistant strain compared with the reference drug. Compounds 5 and 7, which contained the most basic substituents—pyrrolidine and piperidine—in their structure, strongly inhibited the growth of the standard strain (MIC 2 µg/mL). Furthermore, the same derivatives exhibited activity comparable to that of the reference drugs against some types of Gram-positive bacteria (MIC 0.49 µg/mL) and showed no cytotoxicity (IC50 > 50 µg/mL) in HaCaT cells. The zwitterionic structure of each compound was determined using X-ray crystallography. Absorption, distribution, metabolism, and excretion analyses showed that all compounds are good drug candidates. Thus, compounds 5 and 7 were identified as leading structures for further research on antituberculosis drugs with extended effects. Full article
(This article belongs to the Special Issue Organic Compounds and Nanoparticles Studies for Applications in Cancer and Tuberculosis Therapeutics)
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16 pages, 4991 KiB  
Article
N′-Substituted 4-Phenylpicolinohydrazonamides with Thiosemicarbazone Moiety as New Potential Antitubercular Agents: Synthesis, Structure and Evaluation of Antimicrobial Activity
by Katarzyna Gobis, Małgorzata Szczesio, Andrzej Olczak, Ida Mazerant-Politowicz, Dagmara Ziembicka, Barbara Pacholczyk-Sienicka, Ewa Augustynowicz-Kopeć, Agnieszka Głogowska, Izabela Korona-Głowniak and Andrzej Fruziński
Materials 2022, 15(16), 5513; https://doi.org/10.3390/ma15165513 - 11 Aug 2022
Cited by 4 | Viewed by 1251
Abstract
Three new 4-phenylpicolin derivatives with a thiosemicarbazone structure were synthesized and evaluated for tuberculostatic activity. The compounds were obtained by the condensation of methyl 4-phenylpicolonimidate with the corresponding cycloalkylamino-1-carbothiohydrazides. The 1H NMR temperature spectra obtained showed proton lability at the nitrogen atom [...] Read more.
Three new 4-phenylpicolin derivatives with a thiosemicarbazone structure were synthesized and evaluated for tuberculostatic activity. The compounds were obtained by the condensation of methyl 4-phenylpicolonimidate with the corresponding cycloalkylamino-1-carbothiohydrazides. The 1H NMR temperature spectra obtained showed proton lability at the nitrogen atom N2, and X-ray crystallography confirmed the zwitterionic structure of all products. ADME calculations indicate that the compounds can be tested as future drugs. All compounds were absorbed in the gastrointestinal tract. All compounds also showed very good tuberculostatic activity (MIC 3.1–12.5 µg/mL). Derivative 1b showed the best selectivity for M. tuberculosis compared to the other pathogenic species tested. The study has allowed the emergence of imine derivative 1b as a good structure for further optimization in the search for antitubercular drugs. Full article
(This article belongs to the Special Issue Organic Compounds and Nanoparticles Studies for Applications in Cancer and Tuberculosis Therapeutics)
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