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Pyranopyrazoles as efficient antimicrobial agents: Green, one pot and multicomponent approach
Guda Mallikarjuna Reddy1, Jarem Raul Garcia2, Grigory V Zyryanov3
1Ural Federal University, Chemical Engineering Institute, Yekaterinburg 620002, Russia; Department of Chemistry, State University of Ponta Grossa, Ponta Grossa, Parana State, Brazil.
Bioorganic Chemistry
|November 12, 2018
Summary
Researchers developed novel therapeutic heterocycles using an eco-friendly method. Compound 6f showed excellent antimicrobial activity against pathogens, suggesting potential for new drug development.
Area of Science:
- Medicinal Chemistry
- Organic Synthesis
- Antimicrobial Agents
Background:
- Heterocyclic compounds are crucial in drug discovery.
- Developing novel antimicrobial agents is a global health priority.
- Eco-friendly synthetic routes are essential for sustainable chemistry.
Purpose of the Study:
- To synthesize novel thiadiazolyl-pyranopyrazole heterocycles.
- To evaluate the antimicrobial and antifungal activities of synthesized compounds.
- To investigate structure-activity relationships (SARs) for antimicrobial efficacy.
Main Methods:
- Green synthesis of thiadiazolyl-pyranopyrazole derivatives.
- Antimicrobial susceptibility testing against four bacterial and two fungal strains.
- Determination of minimum inhibitory concentration (MIC) and minimum bactericidal/fungicidal concentration (MBC/MFC).
Main Results:
- All synthesized compounds were obtained in quantitative yields.
- Compound 6f exhibited potent broad-spectrum antimicrobial activity.
- Compounds 6d, 6g, and 6l showed promising antimicrobial results.
- Active compounds demonstrated greater efficacy against Gram-negative bacteria and A. niger.
- Compounds 6j and 6k displayed no activity against tested strains.
Conclusions:
- The green synthetic approach is effective for generating biologically active heterocycles.
- Compound 6f is a promising lead candidate for novel antimicrobial drug development.
- Further preclinical investigations are warranted for these potent antimicrobial motifs.
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