Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors.
The optimization of GS39783 into potent, selective, and safe positive allosteric modulators of GABA(B) receptors is presented.
Guery
Sébastien
S
Novartis Institutes for Biomedical Research, Neuroscience, Novartis Pharma A.G., Basel, Switzerland. sebastien.2.guery@gsk.com
Floersheim
Philipp
P
Kaupmann
Klemens
K
Froestl
Wolfgang
W
D000494:Allosteric Regulation; D003517:Cyclopentanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018080:Receptors, GABA-B / Q000737:chemistry / Q000187:drug effects*; D013329:Structure-Activity Relationship
D003517:Cyclopentanes; C478058:N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine; D011743:Pyrimidines; D018080:Receptors, GABA-B