Basic 3-hydroxypyridin-4-ones: Potential antimalarial agents

Dehkordi, Lotfollah S.; Liu, Zu D.; Hider, Robert C.

doi:10.1016/j.ejmech.2007.07.011

Cited by 44 publications

(32 citation statements)

References 27 publications

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“…They are good ligands for the nucleophilic and electrophilic substitution reactions (Ichimoto and Tatsumi, 1965;Uher et al, 2000). Therefore, many researchers used them for starting or intermediate material for preparation of new compounds (O'brien et al, 1960;Ichimoto and Tatsumi, 1965;Ellis et al, 1996;Aytemir et al, 2003Aytemir et al, , 2004Dehkordi et al, 2008). In this study, chlorokojic acid was used as the starting material.…”

Section: Resultsmentioning

confidence: 99%

Synthesis and biological activities of new Mannich bases of chlorokojic acid derivatives

Aytemir

Özçelık

2010

Med Chem Res

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A novel series of 6-chloromethyl-3-hydroxy-2-substituted 4H-pyran-4-one derivatives were synthesized and tested for their antibacterial, antifungal and antiviral in vitro properties. In the view of activity results, compounds 8-11 (MIC: 8 lg/ml) were more remarkably active against Staphylococcus aureus and Enterococcus faecalis. Compounds 1-7 were highly active against Candida albicans and C. parapsilosis with MIC value of 8 lg/ml. Compound 9 bearing 3-chlorophenyl moiety was determined to be the most active compound against RNA virus PI-3.

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Section: Resultsmentioning

confidence: 99%

Synthesis and biological activities of new Mannich bases of chlorokojic acid derivatives

Aytemir

Özçelık

2010

Med Chem Res

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“…Many bacteria synthesize small molecules known as siderophores, which possess high affinity to iron and scavenge it from the environment [3]. 3-Hydroxypyridine-4-one derivatives and their oxygen-containing analogues, 3-hydroxypyran-4-ones, belong to a class of iron chelators with reported in vitro antibacterial, antifungal and antimalarial activities [4][5][6][7]. They have shown inhibitory effects on the growth of Escherichia coli, Listeria inocua and Staphylococcus aureus [8][9][10].…”

Section: Introductionmentioning

confidence: 99%

Computer-aided design of novel antibacterial 3-hydroxypyridine-4-ones: application of QSAR methods based on the MOLMAP approach

Sabet

Fassihi

Hemmateenejad

et al. 2012

J Comput Aided Mol Des

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3-Hydroxypyridine-4-one derivatives have shown good inhibitory activity against bacterial strains. In this work we report the application of MOLMAP descriptors based on empirical physicochemical properties with genetic algorithm partial least squares (GA-PLS) and counter propagation artificial neural networks (CP-ANN) methods to propose some novel 3-hydroxypyridine-4-one derivatives with improved antibacterial activity against Staphylococcus aureus. A large collection of 302 novel derivatives of this chemical scaffold was selected for this purpose. The activity classes of these compounds were determined using the two quantitative structure activity relationships models. To evaluate the predictability and accuracy of the obtained models, nineteen compounds belonging to all three activity classes were prepared and the activity of them was determined against S. aureus. Comparing the experimental results and the predicted activity classes revealed the accuracy of the obtained models. Seventeen of the nineteen synthesized molecules were correctly predicted by GA-PLS model according to the antimicrobial evaluation method. Molecules 5f and 5h proved to be moderately active and active experimentally, but were predicted as inactive and moderately active compounds, respectively by this model. The CP-ANN based prediction was correct for sixteen out of the nineteen synthesized molecules. 5a, 5h and 5q were moderately active and active based on the antimicrobial assays, but they were introduced as members of inactive, moderately active and inactive classes of compounds, respectively according to CP-ANN model.

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“…Od ostalih vrsta bioloških aktivnosti koju pokazuju derivati 3,4-HP treba još spomenuti antimalarijsku, 36 antibakterijsku 37 te antiadhezijsku 4 aktivnost. Pokazalo se da ti spojevi mogu inhibirati rast mnogih bakterija te da je, osim sposobnosti keliranja željeza, nekoliko dodatnih strukturnih faktora važno u pokazivanju navedenog učinka.…”

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“…Neki od njih pokazali su se uspješnima in vitro i in vivo s vrijednostima infektivnih doza ID 50 15 -45 µM, ovisno o derivatu. 36 …”

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3-Hidroksipiridin-4-oni (II. dio): Biološka primjena kao kelatora željeza

et al. 2017

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Basic 3-hydroxypyridin-4-ones: Potential antimalarial agents

Cited by 44 publications

References 27 publications

Synthesis and biological activities of new Mannich bases of chlorokojic acid derivatives

Synthesis and biological activities of new Mannich bases of chlorokojic acid derivatives

Computer-aided design of novel antibacterial 3-hydroxypyridine-4-ones: application of QSAR methods based on the MOLMAP approach

3-Hidroksipiridin-4-oni (II. dio): Biološka primjena kao kelatora željeza

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