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Home Farmaceutický obzor 2009 8-9/2009 4-Chinolóny: výskyt v prírode, možnosti aplikácií a syntetického využitia

4-Chinolóny: výskyt v prírode, možnosti aplikácií a syntetického využitia

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4-Quinolones represent a large group of compounds belonging to tautomeric systems representing hydroxyquinoline - quinolone equilibria1:
Many 4-quinolones are biologically active and therefore some of them were found in nature in some parts of plants or animals, such as zoochromes (uranidine) or alkaloids2,3. In the 70-ties three generations of bactericides were developed. Newer applications are in anticancer therapy exploiting their antitumor activity of cancer of lungs, large intestine, CNS, ovary, breasts, prostate glands etc; but also antihelminthics, antirheumatics, antiameabics, gastric and neurodegenerative diseases (epilepsy, stroke, heart attack, Alzheimer´s disease), antiallergics, antiherpe-tics, SARS treatment, coccidiostatics3.

Primary quinolone could be derivatized by alkyla-tion and saponification (or reversed) and following amination: Chlorination of primary quinolone gives tise to a very reactive a-chloroester system, which allowed us to prepare condensed tri- to pentacyclic systems with fused furo-, thieno-, pyrrolo-, pyrazolo-, pyrimidino-, pyridopyrimido-, benzimidazolo- and triazoloquinolone tautomeric systems4.

Author thanks the Slovak grant agency for financial supports (grants No. 1/9254/02 a 10058/03).

1. Elguero J., Marzin C., Katritzky A.R., Linda P.: Tautomerism of Heterocycles, Adv. Heterocycl. Chem., Suppl. 1, Academic Press, New York 1976.
2. Milata V.: Chemická štruktúra chinolónov a ich antibakteriálna aktivita. II. 4-Chinolóny - ich výskyt v prírode a biologické vlastnosti, Česká a slovenská farmacie, 49(2), 68 (2000).
3. Milata V., Claramunt R.M., Elguero J., P. Zálupský: Chemical Structure and Antibacterial Activity of 4-Quinolones: Incidence in Nature, Preparations and Properties, Targets in Heterocyclic Systems, 4, 167-203 (2000) and citations therein.
4. Milata V., Saloň J., Černuchová P.: unpublished results.





Posledná úprava Utorok, 08 Jún 2010 12:28  

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