The in vitro transport of model thiodipeptide prodrugs designed to target the intestinal oligopeptide transporter, PepT1
A thiodipeptide carrier system is shown to be effective at enabling a range of covalently bound molecules, including benzyl, benzoyl and ibuprofen conjugates, to be transported via the intestinal peptide transporter PepT1, demonstrating its potential as a rational drug delivery target.
Foley, David,Pieri, Myrtani,Pettecrew, Rachel,Price, Richard,Miles, Stephen,Lam, Ho Kam,Bailey, Patrick,Meredith, David
supporting information; experimental part
p. 3652 - 3656
(2009/10/23)
Efficient synthesis of polyfunctionalised enantiopure diazepanone scaffolds
The synthesis of polyfunctionalised enantiopure 1,4-diazepan-3-one scaffolds from l-serine derivatives and azidoepoxides readily available from either l-ascorbic or d-isoascorbic acid, allowing access to various configurations at chiral centres, is descri
Chemical investigations in the synthesis of O-serinyl aminoribosides
Glycosylation involving d-ribose derivatives and various N-protected tert-butyl l-serinates can be achieved efficiently by careful choice of the activation method at the anomeric position and of the Lewis acid promoter. The conditions described allow the major formation of the β-anomer required for further elaboration to liposidomycin and caprazamycin analogues.
Introduction of the Aib-Pro unit into peptides by means of the 'azirine/oxazolone method' on solid phase
A method for the direct introduction of Aib-Pro into peptides on solid phase was developed. The Aib-Pro unit was introduced by means of the 'azirine/oxazolone method' using allyl N-(2,2-dimethyl-2H-azirin-3-yl)-l-prolinate as the synthon. After the reacti
Novel 2-(azetidin-2-on-1-yl)alkanedioic acids and derivatives thereof are described. Methods for using 2-(azetidin-2-on-l-yl)alkanedioic acids and derivatives thereof in the treatment of disease states responsive to antagonism of the vasopressin V1a
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Page/Page column 43
(2008/06/13)
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