Article

Synthesis, Characterization, and in vitro Antimicrobial Screening of Some “1H-Pyrazole’s and 4H-Chromen-4-One’s Derivatives with Penta- Fluoro-Benzoic Acid and 2,3,4,5-Tetra-Fluoro-Benzoic Acid”

Rohit Jaysing Bhor1★, Karan Suresh Kadam1, Gaikwad Mayur Sitaram1★ Corresponding author

  1. 1Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy Pravaranagar, Rahata, Ahmednagar, Maharashtra, INDIA.

CORRESPONDENCE

Rohit Jaysing Bhor

Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy Pravaranagar, Rahata, Ahmednagar, Maharashtra, INDIA.

rohit.bhor69@gmail.com

Received: 19-05-2023; Revised: 24-06-2023; Accepted: 15-07-2023.

Volume 13, Issue 4 · pp. 875–882 · PUBLISHED · DOI: 10.5530/ijpi.13.4.110

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ABSTRACT

Background: The pyrazole nucleus has a five-membered heterocycle with two nitrogen atoms next to one another. The two nitrogen atoms are near in pyrazole nucleus heterocyclic compounds. Chromones are benzoannelated -pyrone-ringed heterocyclic compounds having a single oxygen ring. 4H-chromen-4-one Materials and Methods:All Chromones and Pyrazole derivatives were synthesized by conventional reflux method. 1-(4-chloro-2-h ydroxy-5-methylphenyl)ethanone, penta fluoro benzoic acid, 2, 3, 4, 5-Tetrafluorobenzoic acid, Pyridine, Hydrazine Hydrate, Guanidine Hydrochloride, Ethanol, Con. Hydrochloric acid and Phosphorus oxychloride i.e. POCl3 were used for the synthesis of Chromones and Pyrazole Results:Compared to Ciprofloxacin and Gentamycin, the anti-bacterial results for the substances or their derivatives like 7-chloro-6-methyl-2-(pentafluorophenyl )-4H-chromen-4-one (CC); 5-chloro-4-methyl-2-[5-(pentafluorophenyl)-1H-pyrazol-3-yl] phenol (CD); 5-chloro-2-[2-imino-6-(pentafluorophenyl)-1,2-dihydropyrimidin-4-yl]-4-m ethylphenol (CE); 1-(4-chloro-2-hydroxy-5-methylphenyl)-3-(2,3,4,6-tetrafluorophenyl) propane-1,3-dione (CG); 7-chloro-6-methyl-2-(2,3,4,6-tetrafluorophenyl)-4H-chromen-4-one (CH); 5-chloro-4-methyl-2-[5-(2,3,4,6-tetrafluorophenyl)-1H-pyrazol-3-yl]phenol(CI); 5-chloro-2- [2-imino-6-(2,3,4,6-tetrafluorophenyl)-1,2-dihydropyrimidin-4-yl]-4-methylphenol (CJ) against S. aureus and Pseudomonas aeruginosa. Moreover, the compounds code name like 2-acetyl5-chloro-4-methylphenyl pentafluorobenzoate (CA); 1-(4-chloro-2-hydroxy-5-methylphenyl)- 3-(pentafluorophenyl) propane-1,3-dione: (CB); 2-acetyl-5-chloro-4-methylphenyl 2,3,4,6-tetrafluorobenzoate (CF); 1-(4-chloro-2-hydroxy-5-methylphenyl)-3-(2,3,4,6- tetrafluorophenyl)propane-1,3-dione (CG) a derivatives gives potent anti-bacterial activity against Escherichia coli. Conclusion:The title compounds’ and its derivatives’ in vitro antibacterial activity against a few human pathogenic pathogens were investigated. Gram-positive Gram-negative Pseudomonas aeruginosa and Escherichia coli, along with Staphylococcus aureus, are the bacteria. Studies on the link between structure and activity have shown that compounds containing chromones and derivatives of the pyrazole had higher activity than those containing electron-donating groups.

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    Bhor, R. J., Kadam, K. S., & Sitaram, G. M. (). Synthesis, Characterization, and in vitro Antimicrobial Screening of Some “1H-Pyrazole’s and 4H-Chromen-4-One’s Derivatives with Penta- Fluoro-Benzoic Acid and 2,3,4,5-Tetra-Fluoro-Benzoic Acid”. International Journal of Pharmaceutical Investigation, 13(4), 875–882. https://doi.org/10.5530/ijpi.13.4.110