(3R*,4R*,5S*)-4-(4-Methyl­phen­yl)-2,3-diphenyl-7-[(R*)-1-phenyl­ethyl]-1-oxa-2,7-diaza­spiro­[4.5]decan-10-one oxime

In the title compound, C34H35N3O2, the polysubstituted piperidine ring adopts a chair conformation and the isoxazolidine ring is in an envelope form. The mol­ecules are linked into a chain along the b axis by O—H⋯N, C—H⋯O and C—H⋯N inter­actions. The chains are cross-linked via weak C—H⋯π inter­actions

Glucosyl Platinum(II) Complexes Inhibit Aggregation of the C-Terminal Region of the Aβ Peptide

Neurodegenerative diseases are often caused by uncontrolled amyloid aggregation. Hence, many drug discovery processes are oriented to evaluate new compounds that are able to modulate self-recognition mechanisms. Herein, two related glycoconjugate pentacoordinate Pt(II) complexes were analyzed in their capacity to affect the self-aggregation processes of two amyloidogenic fragments, Aβ21-40 and Aβ25-35, of the C-terminal region of the β-amyloid (Aβ) peptide, the major component of Alzheimerʼs disease (AD) neuronal plaques. The most water-soluble complex, 1Ptdep, is able to bind both fragments and to deeply influence the morphology of peptide aggregates. Thioflavin T (ThT) binding assays, electrospray ionization mass spectrometry (ESI-MS), and ultraviolet-visible (UV-vis) absorption spectroscopy indicated that 1Ptdep shows different kinetics and mechanisms of inhibition toward the two sequences and demonstrated that the peptide aggregation inhibition is associated with a direct coordinative bond of the compound metal center to the peptides. These data support the in vitro ability of pentacoordinate Pt(II) complexes to inhibit the formation of amyloid aggregates and pave the way for the application of this class of compounds as potential neurotherapeutics

Microwave mediated synthesis of spiro-(indoline-isoxazolidines): mechanistic study and biological activity evaluation

Regioisomeric spiro-(indoline-isoxazolidines) have been synthesized in moderate yields by the cycloaddition reaction between ethyl (3-indolylidene)acetate and various Substituted alpha,N-diplienylnitrones, using environmentally benign microwave technology. A novel concerted reaction mechanism is described that explains the preferential formation of the regioisomeric spiro-(indoline-isoxazolidine) analogs 6 over 5. These compounds were screened for anti-mycobacterial and anti-invasive activities against tumor cells. (c) 2005 Elsevier Ltd. All rights reserved