Neticonazole Hydrochloride

An otherwise healthy 3-year-old girl presented with a several-month history of scaly lesions on her palms and soles. The lesions on the palms and right sole had been successfully treated with a steroid for pompholyx by a nearby dermatology clinic, but the lesion on the left sole persisted and spread to the back of the foot. On the initial visit, the patient exhibited an itchy and scaly erythematous left foot lesion. Direct microscopic examination of the scales revealed a considerable amount of fungal elements. A diagnosis of tinea pedis was made, and antifungal treatment with a neticonazole ointment was initiated. Complete cure was achieved after 4 weeks of treatment. The primary mycological cultures from the scales simultaneously revealed two types of colonies: a white powdery flat colony and a white downy elevated colony with a reddish-yellow bottom. Although the powdery colony was identified as Trichophyton mentagrophytes complex on slide culture, the downy colonies could not be identified based on cultural and morphological characteristics. The nucleotide sequences of the internal transcribed spacer region from both colonies showed an exact match, which eventually led to their identification as Trichophyton interdigitale. Further genotyping at three points in the non-transcribed spacer region in both colonies also showed the same NTS type of D2II. It is very rare for two morphologically different colonies to be isolated from the primary culture under the same conditions in tinea cases. Genetic tests are of extreme value to identify the strain in such cases.

The constitutive androstane receptor (CAR; NR1I3) is a nuclear receptor involved in all phases of drug metabolism and disposition. However, recently it’s been implicated in energy metabolism, tumor progression, and cancer therapy as well. It is, therefore, important to identify compounds that induce human CAR (hCAR) activation to predict drug-drug interactions and potential therapeutic usage. In this study, we screen the Tox21 10,000 compound collection to characterize hCAR activators. A potential novel structural cluster of compounds was identified, which included nitazoxanide and tenonitrozole, whereas known structural clusters, such as flavones and prazoles, were also detected. Four compounds, neticonazole, diphenamid, phenothrin, and rimcazole, have been identified as novel hCAR activators, one of which, rimcazole, shows potential selectivity toward hCAR over its sister receptor, the pregnane X receptor (PXR). All 4 compounds translocated hCAR from the cytoplasm into the nucleus demonstrating the first step to CAR activation. Profiling these compounds as hCAR activators would enable an estimation of drug-drug interactions, as well as identify prospective therapeutically beneficial drugs.