181484-89-9Relevant articles and documents
Synthesis of potent inhibitors of histidinol dehydrogenase
Dancer, Jane E.,Ford, Mark J.,Hamilton, Kenneth,Kilkelly, Michael,Lindell, Stephen D.,O'Mahony, Mary J.,Saville-Stones, Elizabeth A.
, p. 2131 - 2136 (1996)
Novel inhibitors of histidinol dehydrogenase are described. The most potent inhibitors, compounds 18 (K(i)* = 4.4 nM) and 19 (K(i)* = 2.9 nM) exploit a hitherto unreported lipophilic binding pocket adjoining the active site. Preliminary SAR data for this pocket are detailed. The electrophilic ketone 6 designed to bind to an active site nucleophile was a considerably weaker inhibitor (IC50 ~ 20 μM).