Synthesis and pharmacological evaluation of new compounds with a potential action on the adrenergic system.

A series of compounds with a potential activity on both alpha and beta-adrenoreceptors were synthesized and evaluated with in vitro and in vivo tests. Aryloxypropanolamino derivatives N-substituted with alpha 2-benzodioxanylmethyl group showed a favourable alpha/beta ratio and a high selectivity towards beta 1 receptors. Substitution with different aralkyl groups afforded compounds with a low alpha-activity, although with a high potency and selectivity towards beta 1 receptors.

Synthesis and antibacterial activity of some derivatives of tolypomycinone. Relationship between structure and activity in ansamycins.

3-Aminotolypomycinoes and 3,16-diamino-16,17-dihydrotolypomycinones are formed by the addition of primary and secondary amines to tolypomycinone, obtained by mild hydrolysis of the antibiotic tolypomycin Y.3-Amino-16,17-dihydrotolypomycinones are formed by the addition of primary and secondary amines to 16,17-dihydrotolypomycinone. In vitro microbiological tests showed high antibacterial activity in compounds obtained by the addition of primary amines, which must be unbranched in the alpha position to the nitrogen atom to position 3 of the naphthoquinone ring.