N4-phenyl modifications of N2-(2-hydroxyl)ethyl-6-(pyrrolidin-1-yl)-1,3,5-triazine-2,4-diamines enhance glucocerebrosidase inhibition by small molecules with potential as chemical chaperones for Gaucher disease.
A series of 1,3,5-triazine-2,4,6-triamines were prepared and analyzed as inhibitors of glucocerebrosidase. Synthesis, structure activity relationships and the selectivity of chosen analogues against related sugar hydrolases enzymes are described.
Huang
Wenwei
W
NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Drive, MSC 3370, Bethesda, MD 20892-3370, USA.
Zheng
Wei
W
Urban
Daniel J
DJ
Inglese
James
J
Sidransky
Ellen
E
Austin
Christopher P
CP
Thomas
Craig J
CJ
D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D005776:Gaucher Disease / Q000201:enzymology*; D005962:Glucosylceramidase / Q000037:antagonists & inhibitors*; D006801:Humans; D014227:Triazines / Q000737:chemistry* / Q000494:pharmacology*