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Tropical Journal of Pharmaceutical Research
Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria
ISSN: 1596-5996
EISSN: 1596-9827
Vol. 15, No. 10, 2016, pp. 2197-2207
Bioline Code: pr16290
Full paper language: English
Document type: Research Article
Document available free of charge

Tropical Journal of Pharmaceutical Research, Vol. 15, No. 10, 2016, pp. 2197-2207

 en Synthesis, characterization, antimicrobial activity and molecular docking studies of combined pyrazol-barbituric acid pharmacophores
Barakat, Assem; Qahtani, Bandar M Al-; Majid, Abdullah M Al-; Ali, M; Shaik, Mohammed Rafi; Agamy, Mohamed HM Al- & Wadood, Abdul

Abstract

Purpose: To synthesize, and determine the antibacterial activity and binding mode of new pyrazolbarbituric acid derivatives in a search for new antimicrobial agents.
Methods: One-pot multi-component reaction of aldehyde derivatives, barbituric acid and 3-methyl-1-phenyl-1H-pyrazol-5(4H)-one in the presence of NHEt2 to afford Michael adduct was carried out. The reaction was carried out in water and afforded new heterocycles in a one-step fashion, with expedient work-up and high yield without extraction and purification steps. The synthesized compounds were evaluated for antimicrobial activity using agar disc diffusion. Molecular docking approach via MOE-Dock program was applied to predict the binding interactions of some of the new pyrazol-barbituric acid derivatives against six different target proteins downloaded from Protein Data Bank.
Results: A series of pyrazole-barbituric acid derivatives were successfully synthesized and characterized. The synthesized compounds showed moderate to very good antibacterial activity against S. aureus ATCC 29213 and E. faecalis ATCC29212, as well as also antifungal activity against Candida albicans check for this species in other resources ATCC 10400
Conclusion: A series of pyrazole-barbituric acid derivatives has been synthesized and some of them display antimicrobial activities.

Keywords
Pyrazole; Barbituric acid; Pyrazole-barbituric acid derivatives; Antimicrobial activity; Molecular docking

 
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