 |
PDBsum entry 5t6h
|
|
|
|
References listed in PDB file
|
 |
|
Key reference
|
|
|
Title
|
|
Design and synthesis of brain penetrant trypanocidal n-Myristoyltransferase inhibitors.
|
|
|
Authors
|
|
T.Bayliss,
D.A.Robinson,
V.C.Smith,
S.Brand,
S.P.Mcelroy,
L.S.Torrie,
C.Mpamhanga,
S.Norval,
L.Stojanovski,
R.Brenk,
J.A.Frearson,
K.D.Read,
I.H.Gilbert,
P.G.Wyatt.
|
|
|
Ref.
|
|
J Med Chem, 2017,
60,
9790-9806.
|
|
|
PubMed id
|
|
|
|
|
|
|
|
|
Abstract
|
|
|
N-Myristoyltransferase (NMT) represents a promising drug target within the
parasitic protozoa Trypanosoma brucei (T. brucei), the causative agent for human
African trypanosomiasis (HAT) or sleeping sickness. We have previously validated
T. brucei NMT as a promising druggable target for the treatment of HAT in both
stages 1 and 2 of the disease. We report on the use of the previously reported
DDD85646 (1) as a starting point for the design of a class of potent, brain
penetrant inhibitors of T. brucei NMT.
|
|
|
|
|
|
|
