Pyranopyrazoles as efficient antimicrobial agents: Green, one pot and multicomponent approach.
Anti-Bacterial Agents
/ chemical synthesis
Antifungal Agents
/ chemical synthesis
Aspergillus flavus
/ drug effects
Aspergillus niger
/ drug effects
Bacillus subtilis
/ drug effects
Bentonite
/ chemistry
Escherichia coli
/ drug effects
Green Chemistry Technology
/ methods
Microbial Sensitivity Tests
Molecular Structure
Proteus vulgaris
/ drug effects
Pyrans
/ chemical synthesis
Pyrazoles
/ chemical synthesis
Staphylococcus aureus
/ drug effects
Structure-Activity Relationship
Antimicrobial activity
Ecofriendly solvent
Green synthesis
MIC(MBC/MFC)
SARs
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
02 2019
02 2019
Historique:
received:
21
08
2018
accepted:
24
09
2018
pubmed:
12
11
2018
medline:
31
8
2019
entrez:
12
11
2018
Statut:
ppublish
Résumé
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.
Identifiants
pubmed: 30415166
pii: S0045-2068(18)30912-X
doi: 10.1016/j.bioorg.2018.09.035
pii:
doi:
Substances chimiques
Anti-Bacterial Agents
0
Antifungal Agents
0
Pyrans
0
Pyrazoles
0
Bentonite
1302-78-9
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
324-331Informations de copyright
Copyright © 2018 Elsevier Inc. All rights reserved.