Periphery Exploration around 2,6-Diazaspiro[3.4]octane Core Identifies a Potent Nitrofuran Antitubercular Lead

A small set of twelve compounds of a nitrofuran carboxamide chemotype was elaborated from a readily available 2,6-diazaspiro[3.4]octane building block, exploring diverse variants of the molecular periphery, including various azole substituents. The in vitro inhibitory activities of the synthesized c...

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Autores principales: Lukin, Alexei, Komarova, Kristina, Vinogradova, Lyubov, Dogonadze, Marine, Vinogradova, Tatiana, Yablonsky, Piotr, Kazantsev, Alexander, Krasavin, Mikhail
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10056547/
https://www.ncbi.nlm.nih.gov/pubmed/36985501
http://dx.doi.org/10.3390/molecules28062529
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author Lukin, Alexei
Komarova, Kristina
Vinogradova, Lyubov
Dogonadze, Marine
Vinogradova, Tatiana
Yablonsky, Piotr
Kazantsev, Alexander
Krasavin, Mikhail
author_facet Lukin, Alexei
Komarova, Kristina
Vinogradova, Lyubov
Dogonadze, Marine
Vinogradova, Tatiana
Yablonsky, Piotr
Kazantsev, Alexander
Krasavin, Mikhail
author_sort Lukin, Alexei
collection PubMed
description A small set of twelve compounds of a nitrofuran carboxamide chemotype was elaborated from a readily available 2,6-diazaspiro[3.4]octane building block, exploring diverse variants of the molecular periphery, including various azole substituents. The in vitro inhibitory activities of the synthesized compounds were assessed against Mycobacterium tuberculosis H37Rv. As a result, a remarkably potent antitubercular lead displaying a minimal inhibitory concentration of 0.016 μg/mL was identified.
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spelling pubmed-100565472023-03-30 Periphery Exploration around 2,6-Diazaspiro[3.4]octane Core Identifies a Potent Nitrofuran Antitubercular Lead Lukin, Alexei Komarova, Kristina Vinogradova, Lyubov Dogonadze, Marine Vinogradova, Tatiana Yablonsky, Piotr Kazantsev, Alexander Krasavin, Mikhail Molecules Article A small set of twelve compounds of a nitrofuran carboxamide chemotype was elaborated from a readily available 2,6-diazaspiro[3.4]octane building block, exploring diverse variants of the molecular periphery, including various azole substituents. The in vitro inhibitory activities of the synthesized compounds were assessed against Mycobacterium tuberculosis H37Rv. As a result, a remarkably potent antitubercular lead displaying a minimal inhibitory concentration of 0.016 μg/mL was identified. MDPI 2023-03-10 /pmc/articles/PMC10056547/ /pubmed/36985501 http://dx.doi.org/10.3390/molecules28062529 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Lukin, Alexei
Komarova, Kristina
Vinogradova, Lyubov
Dogonadze, Marine
Vinogradova, Tatiana
Yablonsky, Piotr
Kazantsev, Alexander
Krasavin, Mikhail
Periphery Exploration around 2,6-Diazaspiro[3.4]octane Core Identifies a Potent Nitrofuran Antitubercular Lead
title Periphery Exploration around 2,6-Diazaspiro[3.4]octane Core Identifies a Potent Nitrofuran Antitubercular Lead
title_full Periphery Exploration around 2,6-Diazaspiro[3.4]octane Core Identifies a Potent Nitrofuran Antitubercular Lead
title_fullStr Periphery Exploration around 2,6-Diazaspiro[3.4]octane Core Identifies a Potent Nitrofuran Antitubercular Lead
title_full_unstemmed Periphery Exploration around 2,6-Diazaspiro[3.4]octane Core Identifies a Potent Nitrofuran Antitubercular Lead
title_short Periphery Exploration around 2,6-Diazaspiro[3.4]octane Core Identifies a Potent Nitrofuran Antitubercular Lead
title_sort periphery exploration around 2,6-diazaspiro[3.4]octane core identifies a potent nitrofuran antitubercular lead
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10056547/
https://www.ncbi.nlm.nih.gov/pubmed/36985501
http://dx.doi.org/10.3390/molecules28062529
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