Pyranopyrazoles as efficient antimicrobial agents: Green, one pot and multicomponent approach.

Autor: Reddy GM; Ural Federal University, Chemical Engineering Institute, Yekaterinburg 620002, Russia; Department of Chemistry, State University of Ponta Grossa, Ponta Grossa, Parana State, Brazil., Garcia JR; Department of Chemistry, State University of Ponta Grossa, Ponta Grossa, Parana State, Brazil. Electronic address: nagareddy.organic@gmail.com., Zyryanov GV; Ural Federal University, Chemical Engineering Institute, Yekaterinburg 620002, Russia; Ural Division of the Russian Academy of Sciences, I. Ya. Postovskiy Institute of Organic Synthesis, 22 S. Kovalevskoy Street, Yekaterinburg, Russia., Sravya G; Ural Federal University, Chemical Engineering Institute, Yekaterinburg 620002, Russia., Reddy NB; Ural Federal University, Chemical Engineering Institute, Yekaterinburg 620002, Russia.
Jazyk: angličtina
Zdroj: Bioorganic chemistry [Bioorg Chem] 2019 Feb; Vol. 82, pp. 324-331. Date of Electronic Publication: 2018 Sep 25.
DOI: 10.1016/j.bioorg.2018.09.035
Abstrakt: Innovative therapeutic heterocycles having precisely thiadiazolyl-pyranopyrazole fragments were prepared by using the ecofriendly synthetic route. Entire compounds formed in quantitative yields. All the composites tested for their antimicrobial effectiveness against four microbial, two beneficial fungi's and accurately measured the minimum inhibitory concentrations (MIC and MBC/MFC), along with some initial structure activity relationships (SARs) also discussed. From the biological outcomes, the motif 6f provided an outstanding activity against all six pathogens. The possible presence of a nitro substituent on this composite may undoubtedly enhance the activity. In addition, amalgams 6d, 6g and 6l displayed promising antimicrobial results. This may be justified to the presence of electron capture group attached to the benzene ring, while the combinations 6j and 6k were zero effect towards all bacterial strains. The other compounds were excellent to low antimicrobial efficiency. The intriguing point was observed that all the active compounds had in common immense antibacterial effectiveness on Gram-negative bacteria than Gram-positive one and more antifungal activity on A. niger compare to other fungus. All things considered and suggested that this outstanding green synthetic approach is used to develop biological active compounds. On top of that, biological results confirmed that these biologically energetic motifs suitable for additional preclinical examine with the aim of standing novel innovative drugs.
(Copyright © 2018 Elsevier Inc. All rights reserved.)
Databáze: MEDLINE
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