Pyranopyrazoles as efficient antimicrobial agents: Green,one pot and multicomponent approach |
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| Institution: | 1. Ural Federal University, Chemical Engineering Institute, Yekaterinburg 620002, Russia;2. Department of Chemistry, State University of Ponta Grossa, Ponta Grossa, Parana State, Brazil;3. Ural Division of the Russian Academy of Sciences, I. Ya. Postovskiy Institute of Organic Synthesis, 22 S. Kovalevskoy Street, Yekaterinburg, Russia;1. Institute of Chemical Engineering, Ural Federal University, 620002 Ekaterinburg, Russian Federation;2. I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, 620990 Ekaterinburg, Russian Federation;1. Department of Chemistry, School of Natural Sciences, National University of Sciences & Technology, H-12, Islamabad, 44000, Pakistan;2. Research Center for Modeling & Simulation, National University of Science & Technology, H-12, Islamabad, 44000, Pakistan;3. Atta-Ur-Rahman School of Applied Sciences and Biotechnology, National University of Science & Technology, H-12, Islamabad, 44000, Pakistan;4. Institute of Environment, Health and Societies, Brunel University London, Uxbridge, UB8 3PH, UK;1. National Engineering Research Center of Pesticide (Tianjin), State Key Laboratory and Institute of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin, 300071, People''s Republic of China;2. Key Laboratory for Water Environment and Resources, Tianjin Normal University, Tianjin, 300387, People''s Republic of China;1. National Engineering Research Center for Process Development of Active Pharmaceutical Ingredients, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, China;2. Key Laboratory for Green Pharmaceutical Technologies and Related Equipment of Ministry of Education, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou 310014, China;1. Department of Chemistry, School of Sciences, Gujarat University, Ahmedabad, Gujarat, India;2. Piramal Enterprise Ltd, Plot No.-18, Pharmez, Matoda Village, Ahmedabad, India;3. Department of Botany, Bioinformatics and Climate Change Impacts Management, School of Sciences, Gujarat University, Ahmedabad, Gujarat, India;4. Microcare Laboratory & Tuberculosis Research Centre, Surat, Gujarat, India;5. Genxplore Diagnostic and Research Centre Pvt. Ltd., Ahmedabad, Gujarat, India;1. Department of Chemistry, Indian Institute of Technology (Banaras Hindu University), Varanasi, 221005, India;2. Department of Chemistry, Prof. Rajendra Singh (Rajju Bhaiya) Institute of Physical Sciences for Study & Research V.B.S. Purvanchal University, Jaunpur, 222003, U.P., India |
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| Abstract: | 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. |
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| Keywords: | Antimicrobial activity MIC(MBC/MFC) SARs Ecofriendly solvent Green synthesis |
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