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Synthesis, Antimicrobial Evaluation and Qsar Study of Some 3-Hydroxypyridine-4-One and 3-Hydroxypyran-4-One Derivatives Publisher Pubmed



Fassihi A1 ; Abedi D2 ; Saghaie L1 ; Sabet R1 ; Fazeli H3 ; Bostaki G1 ; Deilami O1 ; Sadinpour H1
Authors
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Authors Affiliations
  1. 1. Department of Medicinal Chemistry, Faculty of Pharmacy, Isfahan University of Medical Sciences, 81746-73461 Isfahan, Hezar Jerib, Iran
  2. 2. Department of Biotechnology, Faculty of Pharmacy, Isfahan University of Medical Sciences, 81746-73461 Isfahan, Hezar Jerib, Iran
  3. 3. Department of Microbiology, Faculty of Medicine, Isfahan University of Medical Sciences, 81746-73461 Isfahan, Hezar Jerib, Iran

Source: European Journal of Medicinal Chemistry Published:2009


Abstract

A series of Mannich bases of 2-alkyl-3-hydroxy-pyridine-4-ones, namely 2-alkyl-3-hydroxy-5-N-piperidylmethyl or N,N-dialkylaminomethyl pyridine-4-ones 9, 10 and 15-18, two derivatives of N-aryl-2-methyl-3-hydroxy-pyridine-4-ones 19, 20 and two N-alkyl derivatives of maltol, 21 and 22 were prepared. They were screened for their antibacterial and antifungal activities against a variety of microorganisms using micro plate Alamar Blue® assay (MABA) method. Multiple linear regressions (MLR) analysis was performed for the synthesized compounds as well as a series of pyridinone and pyranone derivatives 23-43 which have been synthesized and evaluated for antimicrobial activity by other researchers previously. Studied compounds showed a better quantitative structure-activity relationship (QSAR) model for the antimicrobial activity against Candida albicans and Staphylococcus aureus in comparison with other tested microorganisms. © 2008 Elsevier Masson SAS. All rights reserved.
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