MEDICINAL CHEMISTRY APPLIED TO PROBLEMS PROMINENT IN SENESCENCE

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Two problems which have relevance to aging have been studied. In the field of congeners of catecholamines the following results were obtained: (A) A new series of compounds which selectively destroy beta-adrenoceptors was developed which has indexes about two orders better than previously available compounds. The results suggest that new series will enable selective manipulation of beta-adrenoceptors in brain to be performed in a practical manner. (B) A compound which activates and then attaches itself permanently to beta-adrenoceptors was prepared. Evaluation of this compound indicates that beta-adrenoceptor has intrinsic self-deactivation capacity, i.e. cannot be jammed in activated state. (C) Orientation studies of dopamine confiners were initiated. In the field of solubilizers of lipophilic hormones and drugs the previously developed compounds, hydrophilic derivatives of cyclodextrins, were analyzed thoroughly and prepared in quantity to support two clinical evaluation studies.