Azole derivatives topical

Because of their limited, activity, small spectmm, and side effects, the older topical antimycotics have generally been surpassed by newer antimycotic chemotherapeutic agents. These newer antimycotics for topical use iaclude the imida2ole derivatives clotrimazole, miconazole, econazole, isoconazole, sulconazole, fenticonazole, oxiconazole, bifonazole, butoconazole, ziaoconazole, tioconazole, and the triazole derivative, terconazole (Table 2) (5—7). The iatroduction of the azole derivatives represents a milestone ia the treatment of mycoses. 

Topical azole derivatives include the imidazoles bifonazole, clotrimazole, econazole, ketoconazole, miconazole, oxiconazole, lanoconazole, flutrima-zole and sertaconazole. These drugs show activity against the dermatophytes Epidermophyton, Mi-crosporum and Trichophyton. They are also effective against the yeasts Candida albicans and Pityrospo-rum orbiculare. Local side effects include pruritus, erythema and local irritation. Allergic dermatitis is rare. 

Developmental Topical Antimycotics. Most of the topical antimycotics still being developed are azole derivatives (mostly imidazole), including butoconazole, oxiconazole, omoconazole, zinoconazole, and sulconazole (Fig. 3). Generally speaking, these newer azoles offer no additional therapeutic advantages compared to existing substances. These drugs are already available in certain countries, but are not yet commercialized on a worldwide scale. 

Various reviews have been published about this topic. Jeschke and Leroux [2] pubhshed about the medical apphcation of a-fluorinated ethers. Leroux and Pazenok [1] wrote about the synthesis and the properties of trifluoromethyl ethers. Leroux, Jeschke and Schlosser [3b] reviewed the properties of a-fluorinated ethers, thioethers and amines. The work of Boiko [4a] is dedicated to aromatic and heterocyclic perfluoralkyl sulfides. Vovk and Gakh [4b] gave a detailed review about trifluoro-methoxy containing azoles and azines. This review summarized the literature data on synthesis and biological activity of trifluoromethoxy, difluoromethoxy and a-fluorinated sulfides derivatives of five and six membered heterocycles. 

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