Title of article :
Synthesis and biological evaluation of a 2-aryl polyhydroxylated pyrrolidine alkaloid-based library Original Research Article
Author/Authors :
En-Lun Tsou، نويسنده , , Sih-Yu Chen، نويسنده , , Ming-Hsun Yang، نويسنده , , Shih-Chi Wang، نويسنده , , Ting-Ren Rachel Cheng، نويسنده , , Wei-Chieh Cheng، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2008
Pages :
7
From page :
10198
To page :
10204
Abstract :
Inspired by polyhydroxylated pyrrolidine alkaloid natural products, a 18-membered library of 2-aryl polyhydroxylated pyrrolidines has been efficiently prepared in two or three synthetic steps from the known chiral cyclic nitrones with high yield and purity and excellent stereoselectivity. The inhibitory activity of all these compounds against various glycosidase enzymes was evaluated. Interestingly, 15 and 19 show better inhibitory activities than radicamine A (20) and B (18) against α-glucosidases. The IC50 values of 15 and 19 are 1.1 and 0.5 μM, respectively. In this study, we also discovered the substituent(s) on the aryl ring could affect the inhibition potency and selectivity against glycosidases.
Keywords :
Polyhydroxylated pyrrolidine alkaloid , Natural product-like molecule , Chiral cyclic nitrone , Structural diversity , Glycosidase inhibitors
Journal title :
Bioorganic and Medicinal Chemistry
Serial Year :
2008
Journal title :
Bioorganic and Medicinal Chemistry
Record number :
1306120
Link To Document :
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