TY  - JOUR
A1  - Bajda, Marek
A1  - Wieckowska, Anna
A1  - Hebda, Michalina
A1  - Guzior, Natalia
A1  - Sotriffer, Christoph A.
A1  - Malawska, Barbara
T1  - Structure-Based Search for New Inhibitors of Cholinesterases
JF  - International Journal of Molecular Sciences
N2  - Cholinesterases are important biological targets responsible for regulation of cholinergic transmission, and their inhibitors are used for the treatment of Alzheimer’s disease. To design new cholinesterase inhibitors, of different structure-based design strategies was followed, including the modification of compounds from a previously developed library and a fragment-based design approach. This led to the selection of heterodimeric structures as potential inhibitors. Synthesis and biological evaluation of selected candidates confirmed that the designed compounds were acetylcholinesterase inhibitors with \(IC_{50}\) values in the mid-nanomolar to low micromolar range, and some of them were also butyrylcholinesterase inhibitors.
KW  - fragment-based design
KW  - cholinesterases inhibitors
KW  - butyrylcholinesterase
KW  - acetylcholinesterase
KW  - drug design
Y1  - 2013
U6  - http://nbn-resolving.de/urn/resolver.pl?urn:nbn:de:bvb:20-opus-129423
VL  - 14
IS  - 3
ER  -