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

ABSTRACT: 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.

SUBMITTER: Lukin A

PROVIDER: S-EPMC10056547 | biostudies-literature | 2023 Mar

REPOSITORIES: biostudies-literature

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

Lukin Alexei A Komarova Kristina K Vinogradova Lyubov L Dogonadze Marine M Vinogradova Tatiana T Yablonsky Piotr P Kazantsev Alexander A Krasavin Mikhail M

Molecules (Basel, Switzerland) 20230310 6

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 <i>Mycobacterium tuberculosis</i> H37Rv. As a result, a remarkably potent antitubercular lead displaying a minimal inhibitory concentration of 0.016 μg/mL was identified ...[more]

PMID: 36985501

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