- Synthesis of novel polyhydroxylated pyrrolidine-triazole/-isoxazole hybrid molecules.
Synthesis of novel polyhydroxylated pyrrolidine-triazole/-isoxazole hybrid molecules.
Organic & biomolecular chemistry (2014-12-20)
Cheng-Kun Lin, Li-Wei Cheng, Huang-Yi Li, Wen-Yi Yun, Wei-Chieh Cheng
PMID25525831
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A straightforward synthesis of novel, 2-heterocyclyl polyhydroxylated pyrrolidines is described. Stereocontrolled additions of nucleophiles to cyclic nitrones generated the corresponding 2,3-trans adducts, allowing the synthesis of the corresponding pyrrolidines via key intermediates bearing an alkyne and a nitrile oxide. Three hybrid systems, including a pyrrolidine with two isoxazoles and one triazole, are efficiently prepared via 1,3-dipolar cycloaddition. Biological testing of the product alkaloids showed that subtle structural variations have drastic effects on their inhibitory activities against glucosidases.
MATERIALS
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Sigma-Aldrich
ฮฑ-Glucosidase from Bacillus stearothermophilus, lyophilized powder, โฅ50 units/mg protein