Article
Rapid preparation of (3R,4S,5R) polyhydroxylated pyrrolidine-based libraries to discover a pharmacological chaperone for treatment of Fabry disease.
European journal of medicinal chemistry - 27 Jan 2017
Cheng Wei-Chieh, Wang Jen-Hon, Yun Wen-Yi, Li Huang-Yi, Hu Jia-Ming
Abstract excerpt
The rapid discovery of a pharmacological chaperone toward human α-Gal A for the treatment of Fabry disease is described. Two polyhydroxylated pyrrolidines with the (3R,4S,5R) configuration pattern underwent rapid substituent diversity by conjugating the primary aminomethyl moiety of each with a variety of carboxylic acids to generate two libraries (2 × 60 members). Our bioevaluation results showed one member with...
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