POLYISOPRENOID AMPHIPHILIC COMPOUNDS AS INHIBITORS OF SQUALENE SYNTHESIS AND OTHER MICROSOMAL-ENZYMES

Analogues of farnesyl pyrophosphate containing a farnesyl moiety and a variety of amine residues replacing the pyrophosphate have been synthesized. Most of these compounds were effective inhibitors of the synthesis of squalene and presqualene pyrophosphate from farnesyl pyrophosphate. 50% inhibition was obtained at concentrations between 50 and 100 μM. These analogues also inhibited other microsomal enzymes so they apparently function as general inhibitors of microsomal enzymes. © 1978.