Simple isoquinoline and benzylisoquinoline alkaloids as potential antimicrobial, antimalarial, cytotoxic, and anti-HIV agents

Twenty-six simple isoquinolines and 21 benzylisoquinolines were tested for antimicrobial, antimalarial, cytotoxic, and anti-HIV activities. Some simpl e isoquinoline alkaloids were significantly active in each assay, and may b e useful as lead compounds for developing potential chemotherapeutic agents . These compounds include 13 (antimicrobial), 25, 26, and 42 (antimalarial) , 13 and 25 (cytotoxic), and 28 and 29 (anti-HIV). A quaternary nitrogen at om of isoquinolium or dihydroisoquinolinium type may contribute to enhanced potency in the first three types of activities. In contrast, anti-HIV acti vity was found with tetrahydroisoquinoline and 6,7-dihydroxyisoquinolium sa lts. (C) 2001 Elsevier Science Ltd. All rights reserved.