30652-13-2Relevant articles and documents
Synthesis, antimicrobial evaluation and QSAR study of some 3-hydroxypyridine-4-one and 3-hydroxypyran-4-one derivatives
Fassihi, Afshin,Abedi, Daryoush,Saghaie, Lotfollah,Sabet, Razieh,Fazeli, Hossein,Bostaki, Ghasem,Deilami, Omid,Sadinpour, Hekmatollah
body text, p. 2145 - 2157 (2009/09/30)
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.
Synthesis and in vitro trypanocidal activity of some novel iron chelating agents
Singh, Pramod K.,Jones, Mark M.,Lane, Joshua E.,Nesset, Anna,Zimmerman, Lisa J.,Ribeiro-Rodrigues, Rodrigo,Richter, Ashley,Stenger, Michael R.,Carter, Clint E.
, p. 311 - 315 (2007/10/03)
This report describes the syntheses and in vitro trypanocidal activity of a number of iron(III) chelators against epimastigotes of Trypanosoma cruzi. The compounds examined included a number of lipophilic N-alkyl derivatives of 2-ethyl- and 2-methyl-3-hydroxypyrid-4-ones, N,N'-bis(o-hydroxybenzyl)-(±)-trans-1,2-diaminocyclohexane, cyclotetrachromotropylene and four commercially available carboxy derivatives of pyridine, pyrazine, and pyarazole. Benznidazole, the drug clinically used in the treatment of Chagas' disease in humans, served as standard. All compounds were screened in vitro against Trypanosoma cruzi epimastigotes at 50 and 100 μg/ml for 72 h of exposure. At 100 μg/ml dosage, at least 4 compounds exhibited high epimastigote growth inhibition (65-69%) comparable to benznidazole (72%), whereas 9 compounds showed moderate to fair activity (53-64%) in the in vitro assay. At the lower concentration (50 μg/ml), the inhibitory activity of the best of these compounds was reduced significantly (39-48%) compared to the standard drug (59%). The activity of all the carboxylic acids remained in the lower range (4-25%). It is hypothesized that the enhanced activity of some of the compounds is due to their increased lipophilicity which enables them to successfully pass through the cellular membrane of Trypanosoma cruzi epimastigotes. The trypanocidal activities of the most effective compounds were significantly reduced when tested in the presence of added ferric ion.
5,6-Dihydro-3,5-dihydroxy-4H-pyridones - A new maillard products from 6-O-substituted hexoses and primary amines
Kettner,Ledl,Lerche,Severin
, p. 9351 - 9356 (2007/10/02)
From reaction mixtures of n-propylamine and 6-O-substituted hexoses 1 (glucose-6-phosphate, isomaltose, 6-O-benzylgalactose) a previously unknown Maillard product, the 5,6-dihydro-3,5-dihydroxy-1-n-propyl-4H-pyridone (7a) was isolated in yields up to 20%.