Synthesis and Biological Activities of Griseofulvin Analogs

Abstract

In order to elucidate the structure-activity relationship of griseofulvin (1), (±)-6'-demethyl analog (3), 2'-demethoxy-6'-demethyldihydro analog (4), (±)-dechloro-6'-ethyl analog (5), (±)-dechloro-6'epi-ethyl analog (6), (±)-6'-ethyl analog (7) and (±)-6'-epi-ethyl analog (8) were synthesized by a Diels-Alder cycloaddition of alkylidene ketones (16, 17, 18, 19 and 20) with modified 1, 3-butadienes (21 or 22). Their biological activities were examined against fungi.