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1 Wiadomości Chemiczne

1 2003

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Biologicznie aktywne pochodne 1,8-naftyrydyny

Suryło P., Kowalski P., Hołda M.

Wiadomości Chemiczne

2003

[Z] 57, 3-4

247--266

This review attempts to briefly summarise the recent developments in the synthesis and application of 1,8-naphthyridine derivatives as biological active compounds. A large number of these compounds still evolves interest of chemists and pharmacologists. From among of one thousand papers, which appeared within the last fifteen years, most described applications of 1,8-naphthyridine derivatives as biologicaly active compounds. Nalidixic acid (1) was the first 1,8-naphthyridine derivative approved as the drug with antibacterial activity. There are many routes to the synthesis of nalidixic acid. The main routes are presented in the Schemes 1, 4, and 6. This compound was the first from the quinolone's family applied as the chemotherapeutic drug. Modification of the structure of nalidixic acid brought the discovery of a new group of most potent antibacterial compounds called fluoroquinolones. Enoxacine (16), esafloxacine (21), tosulfoxacine (22), trovafloxacine (23) and alatrofloxacine (24) are the examples of 1,8-naphthyridine derivatives belonging to that group. General reaction scheme of synthesis of 16 and 21 is similar to synthesis of nalidixic acid, while synthesis of the compounds 22, 23, and 24 presented in Scheme 8 is quite different. Moreover, many other 1,8-naphthyridine derivatives 31-40 have been intensively studied as antibacterial agents in vitro, but none of them has been applied as a drug. A number of 2- and 7-substituted 1,8-naphthyridines 41 showed some antimalarial activity in vivo, while the compounds of general structure 42 were found inactive. 2(4)-Piperazinyl-1,8-naphthyridines (45) have been pharmacologically investigated for their antyhipertensive activity. 1,8-Naphthyridines 46, bearing a phenyl group in position 2, were found to be selective antagonists for the A1 adenosine receptor subtype. A series of 1,8-naphthyridines 47-49 exhibited appreciable diuretic and antikaliuretic activity in rats. In search for potential anticancer compounds study such as SAR (structure activity relationship) and QSAR (quantity structure activity relationship) have been used. As the result of the research the structure of the compounds 50 has established as the most potent inhibitor of tubulin polymerization. The nitrobenzo-1,8-naphthyridines (52)constitute a group of potential interest for the design of new cytotoxins. Moreover, 1,8-naphthyridine derivatives have been found to be active as inhibitors of platelet aggregation agents 53-54 ; antiviral 56-57 and antialergic agents 62. These derivatives possess bronchodilating 64, antiflammatory and sedative properties 67.