Lichen planopilaris: report of 30 cases and review of the literature

BACKGROUND: Lichen planopilaris (LPP) affects primarily the scalp, resulting in scaling, atrophy, and alopecia with scarring. The purpose of our study was to obtain original data on LPP and to evaluate the efficacy of topical therapy in comparison with systemic therapies. METHODS: We examined 30 patients affected by LPP between 1996 and 2001, performing clinical, laboratory, histopathologic and direct immunofluorescence examinations. Twenty-one of the patients (70%) were women and nine (30%) were men. The average age at presentation was 51.5 years. The average duration of the disease was 13 months at the time of the diagnosis. All patients received topical steroids for a total of 12 weeks. RESULTS: Resolution of the inflammatory process and blocking of the cicatricial progression were observed in 66% of cases, a mild reduction of fibrosis and cicatrization in 20% of patients, and no response in 13%. CONCLUSIONS: We concluded that topical therapy may be a valid alternative to systemic therapies, especially in patients with lesions in the early phase.     

The role of HB-donor groups in the heterocyclic polar fragment of H3-antagonists. I. Synthesis and biological assays

It has been recently reported that compounds composed of an imidazole connected through an alkyl spacer to a 2-aminobenzimidazole showed high affinity towards the H(3)-receptor. The guanidine fragment of the 2-aminobenzimidazole is probably involved in hydrogen bond interactions at the binding site, and is referred to as the 'polar fragment'. In the present work, starting from 2-aminobenzimidazole derivatives with a di-methylene spacer 1 (pK(i)=7.25) or a tri-methylene one 2 (pK(i)=8.90), we investigated the importance of the hydrogen bond (HB) donor groups at the polar fragment in the interaction with the H(3)-receptor. The replacement of 2-aminobenzimidazoles with different moieties [2-aminobenzothiazole, 3, 4; 2-thiobenzimidazole, 5, 6; 2-thiobenzothiazole, 7, 8; 2-thio-4-phenyl- or 2-thio-5-phenyl-N-methylimidazoles, 9-12] highlighted the effect of the polar group basicity on the optimal length of the alkyl chain: longer spacers were preferred with polar groups of moderate basicity whereas, in the presence of neutral polar groups, the best affinity values were obtained with di-methylene chains. Moreover, N-methylation at the 2-aminobenzimidazole moiety 13-16 revealed different behaviour for compounds having different spacer lengths. In fact, methylation of the exocyclic NH group maintained high affinity for the tri-methylene 2-aminobenzimidazole derivative, while a drop in affinity was observed for the annular N-methylation. An opposite trend characterised di-methylene derivatives. These observed SAR suggest that, within this class of compounds, the number of HB-donor groups can be lowered while maintaining high receptor affinity. Since the presence of HB-donor groups strongly affects brain access, this observation could be useful to design and prepare new H(3)-antagonists.