Privileged structures bind to multiple receptors with high affinity, thus aiding the development of novel biologically active compounds. Indoles are classed as privileged structures, and as a result of the indole nucleus being present in a broad range of biologically active molecules, it has been suggested that indoles probably represent the most important of all structural classes in drug discovery. Amongst the indole class of compounds is a particular subset - 2-arylindoles - which appear to be a most promising lead for drug development. This review summarises the wide-ranging activities of 2-arylindoles and some of their important biological activities reported in the literature over the past two decades.

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Genetic anticipation, manifested by increased severity and earlier age-at-onset of the disease over successive generations, is reported in schizophrenia. The molecular basis of anticipation in several neurodegenerative diseases is unstable coding CAG repeat expansions. Anticipation was reported in schizophrenia. Recently, studies suggested that enlarged CAG/CTG repeats are over represented in schizophrenic patients compared to normal controls. Together, these observations suggest that unstable CAG repeats may play a role in the etiology of schizophrenia. The purpose of this study is to test for the presence of polyglutamineexpanded tracts, encoded by CAG repeats, in total protein extracts derived from lymphoblastoid cell lines of schizophrenic patients. Proteins from schizophrenic patients (n = 59) and normal controls (n = 73) were separated by means of SDS-polyacrylamide gel electrophoresis, wet blotted onto nitrocellulose membrane and probed with a monoclonal antibody (mab 1C2) recognizing expanded polyglutamine arrays. Three abnormal bands corresponding to protein(s) of molecular weight of approximately 50 kDa were identified in two unrelated schizophrenic patients and in a sibling of one of these patients. None of the normal controls tested positive for this abnormal band. These results suggest that expanded polyglutamine-containing proteins, though rare, may play a role in the pathogenesis of schizophrenia.

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Bromhexine, 16 mg. 3-times daily, was compared with placebo in a double-blind crossover trial in 41 out-patients with chronic bronchitis and irreversible airways obstruction, and who were considered to be in a steady state. Each treatment was given for 3 weeks with a week of placebo in between; in addition, all patients took oxytetracycline, 500 mg. twice daily, starting 1 week before the trial and continuing throughout the duration of it. All patients completed the trial but the results from 5 were excluded because during the first 3 weeks they developed an influenza-like illness accompanied by a decrease in FEV1,and peak expiratory flow rate. Results from the remaining 36 patients showed a statistically significant reduction in phlegm stickiness (p smaller than 0.05) as judged by the patient, and a significant improvement in overall clinical state (p smaller than 0.05) as judged by the physician during bromhexine treatment, but no significant change in symptoms like cough, chest tightness, ease of breathing or sputum volume, peak expiratory flow rate and FEV1 etc. Five patients reported 6 side-effects, 3 with bromhexine, 1 with placebo and 1 with both treatments.

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