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Summary
Novelty: Novel naphthylethyl urea and naphthylethyl thiourea derivatives with specific melatonin receptor binding properties are disclosed. They are stated to have anxiolytic, antipsychotic and analgesic properties and ovulation inhibitory and immunomodulatory effects. They are potentially useful for the treatment of a variety of CNS disorders including anxiety, epilepsy, Parkinson's and Alzheimer's disease and sleeping disorders. They also have application in the treatment of hair and skin disorders and to treat some types of tumours.
Biology: Typical melatonin receptor binding assays were carried out in vitro using sheep par tuberalis receptors (Journal of Neuroendocrinology (1989) 1: 1-4). Compounds showed very high specific binding properties with some agents having a 100-fold higher affinity for receptors than melatonin itself (kd∼10-13mol/l compared to 6.3 ± 10-11mol/l for melatonin).
Chemistry: Synthesis by conventional methods is exemplified in twenty-six cases forming a subsidiary part of the claim. N-[2-(7-methoxynaphth-l-yl)-ethyl]N′- propylurea is one of ten specifically claimed compounds.