A 2-methyleneoxetane analog of orlistat demonstrating inhibition of porcine pancreatic lipase

Bioorganic & Medicinal Chemistry Letters
1998.0

Abstract

The 2-methyleneoxetane analog 2 of orlistat (OLS, 1) has been synthesized and tested against porcine pancreatic lipase (PPL). Despite the loss of the carbonyl group, a potential site for hydrogen bonding interaction with the enzyme and the key element in the acylation by OLS, 2 has activity comparable to 1.

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