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The invention provides compds. of formula I, as 11-β-hydroxysteroid dehydrogenase inhibitors (11-β-HSD), which are useful in the treatment of various diseases. Compds. of formula I wherein R1 is (un)substituted fused polycyclic groups, (un)substituted (un)branched alkyl, and (un)substituted cycloalkyl; Z is a carbonyl group or a isostere of a carbonyl group; R2 is (un)substituted arom. ring and (un)substituted heterocyclic ring are claimed in this invention. Example compd. II was prepd. by amidation of adamantane-1-carbonyl chloride with 2-thiophenemethanamine. All the invention compds. were evaluated for their 11-β-HSD inhibitory activity. From the assay, it was detd. that compd. II exhibited 20-60 % inhibition of 11-β-HSD1. [on SciFinder(R)]

Type

Patent

Keywords

adamantanecarboxylic acid deriv prepn hydroxysteroid dehydrogenase inhibitor pharmaceutical compn