Molecules
(Mar 2023)
Periphery Exploration around 2,6-Diazaspiro[3.4]octane Core Identifies a Potent Nitrofuran Antitubercular Lead
Alexei Lukin,
Kristina Komarova,
Lyubov Vinogradova,
Marine Dogonadze,
Tatiana Vinogradova,
Piotr Yablonsky,
Alexander Kazantsev,
Mikhail Krasavin
Affiliations
Alexei Lukin
Lomonosov Institute of Fine Chemical Technologies, MIREA—Russian Technological University, 119454 Moscow, Russia
Kristina Komarova
Lomonosov Institute of Fine Chemical Technologies, MIREA—Russian Technological University, 119454 Moscow, Russia
Lyubov Vinogradova
Lomonosov Institute of Fine Chemical Technologies, MIREA—Russian Technological University, 119454 Moscow, Russia
Marine Dogonadze
Saint Petersburg Research Institute of Phthisiopulmonology, 2-4 Ligovsky Prospekt, 191036 Saint Petersburg, Russia
Tatiana Vinogradova
Saint Petersburg Research Institute of Phthisiopulmonology, 2-4 Ligovsky Prospekt, 191036 Saint Petersburg, Russia
Piotr Yablonsky
Saint Petersburg Research Institute of Phthisiopulmonology, 2-4 Ligovsky Prospekt, 191036 Saint Petersburg, Russia
Alexander Kazantsev
Institute of Chemistry, Saint Petersburg State University, 26 Universitetskii Prospect, 198504 Peterhof, Russia
Mikhail Krasavin
Institute of Chemistry, Saint Petersburg State University, 26 Universitetskii Prospect, 198504 Peterhof, Russia
DOI
https://doi.org/10.3390/molecules28062529
Journal volume & issue
Vol. 28,
no. 6
Abstract
Read online
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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