- N-Oxide as a Potential Function in the Design of Enzyme Inhibitors. Application to 2,3-Epoxysqualene-sterol Cyclases
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The N-oxides of several tertiary amines possessing an aliphatic long chain are more potent inhibitors of 2,3-epoxysqualene-β-amyrin and -lanosterol cyclases than their parent amines.
- Cerutti, Maurizio,Delprino, Laura,Cattel, Luigi,Bouvier-Nave, Pierrette,Duriatti, Albert,et al.
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- Synthesis and biological activity of azasqualenes, bis-azasqualenes and derivatives
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Azasqualenes, bis-azasqualenes and derivatives, designed as inhibitors of squalene 2,3-epoxide cyclase, a key enzyme in sterol biosynthesis, were synthesized and their in vitro activities against a variety of yeasts, fungi, gram-positive and gram-negative bacteria were determined.The synthesis involves a new method of squalene degradation, together with an unusual procedure for the aminative reduction of lipophilic aldehydes.A study of the structure-activity relationship was attempted for different biological parameters: anti-bacterial and anti-fungal activities (MIC), inhibition of mycelial growth (GTT), surfactant activity (CMC) and membrane perturbation activity (induction of leakage in liposomes).
- Ceruti, Maurizio,Balliano, Gianni,Viola, Franca,Cattel, Luigi,Gerst, Nicolas,Schuber, Francis
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p. 199 - 208
(2007/10/02)
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