Sulconazole

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. 

Spiropiperone I, 306 Spirorenone 3, 91, 92 Spi rothiobarbital 1, 276 Stanazole 174 Stenbolone acetate 155 Styramate 2. 219 Succinyl sulfathiazole U 132 Sudoxicam 2, 394 Sulazepam , 403 Sulconazole 3, 133 Sulfabenzamide 112... 

Fenticonazole Isoconazole Miconazole Sertaconazole Sulconazole Tioconazole... 

Aboul-Enein and Ali [78] compared the chiral resolution of miconazole and two other azole compounds by high performance liquid chromatography using normal-phase amylose chiral stationary phases. The resolution of the enantiomers of ( )-econazole, ( )-miconazole, and (i)-sulconazole was achieved on different normal-phase chiral amylose columns, Chiralpak AD, AS, and AR. The mobile phase used was hexane-isopropanol-diethylamine (400 99 1). The flow rates of the mobile phase used were 0.50 and 1 mL/min. The separation factor (a) values for the resolved enantiomers of econazole, miconazole, and sulconazole in the chiral phases were in the range 1.63-1.04 the resolution factors Rs values varied from 5.68 to 0.32. 

If the displacement reaction is carried out between imidazole derivative and thiophene analogue the antifungal agent tiaconazole (40) results. A rather slight variant of this sequence produces antifungal sulconazole (41).Obvious variants of the route explicated above for ketoconazole (34) lead to parconazole (42)and doconazole (43),instead. 

Like econazole, sulconazole is used externally (only superficially) for the same indications as econazole. Synonyms of this drug are exelderm, sulcosyn, and others. 

Miconazole, oxiconazole, ketoconazole, sulconazole, clotrimazole (along with betamethasone dipropionate), terbinafine (SEBIFIN), naftifine, butenafine, tolnaftate, nystatin, amphotericin B, cyclopirox... 

The topical imidazoles, which currently include clotrimazole, econazole, ketoconazole, miconazole, oxiconazole, sulconazole, and sertaconazole, have a wide range of activity against dermatophytes (epidermophyton, microsporum, and trichophyton) and yeasts, including Candida albicans and Pityrosporum orbiculare (see Chapter 48). 

Sulconazole nitrate Exelderm Stearyl alcohol, cetyl alcohol, polysorbate 60, sorbitan monostearate, and PEG-100 stearate None... 

FIGURE 11 Chromatograms of enantiomeric resolution on cellulose tricarbamate CSPs. (a) Econozole. (b) Miconazole, (c) Sulconazole on a Chiralcel OF CSP, with hexane-2-propanol-diethylamine (425 74 1, v/v/v) as the mobile phase, (d) ( )-f/ reoMethyl-phenidate on a Chiralcel OD CSP, with hexane-ethanol-methanol-trifluoroacetic acid (480 9.75 9.75 0.5, v/v/v/v) as the mobile phase. (From Refs. 100, 101.)... 

AD, AS, and AR CSPs by adjusting flow rates. The flow rates were varied between 0.5 and 2.0mL/min, but the best resolution was achieved at a flow rate of 0.5 mL/min. Table 5 shows values for separation factor a and resolution Rs of the antifungal agents at flow rates of 0.5 and 1.0 mL/min. There was no resolution for miconazole and sulconazole, while only partial resolution of econazole was obtained when the flow rate was 1 mL/min. Therefore, a... 

FIGURE 18 Chemical structures of econazole, miconazole, sulconazole, tetralone derivatives, and aromatase inhibitors. 

As in the case of other CSPs, the chiral resolution on these CSPs is also affected by a change in the structures of the racemic compounds. The different selectiv-ities of amino acids on these CSPs may be considerd as the best example. The effect of structures of the racemates on the chiral resolution may be understood from the work carried out by Shieh et al. [71]. The authors studied the chiral resolution of amino acids as their Schiff s bases. These racemates differ slightly in their structure and the substituent, such as alkyl groups, hence showed different values of enantioselectivities. The values of retention and separation factors decreased by introducing bulky groups in the racemates. Aboul-Enein and Ali [70] observed the lower values of retention factors of miconazole in comparison to econazole and sulconazole. The authors explained this sort of behavior on the basis of the steric effect exerted by the extra chlorine atom in miconazole molecule. 

Sulconazole Exelderm Cream solution Tinea (ringworm) infections... 

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