title: Efficient synthesis of phenylene-ethynylene rods and their use as rigid spacers in divalent inhibitors.
abstract: The synthesis of phenylene-ethynylene rods and their use as rigid spacers is described. Alternation of a Sonogashira reaction and silyl group cleavage was used to obtain rigid spacers with even and odd numbers of phenylene units. Preliminary applications of these rods in divalent systems are shown. Inhibition studies with Pseudomonas Aeruginosa lectin LecA showed that the rigid spacer proved greatly beneficial for the inhibitory potency.
authors: Department of Medicinal Chemistry and Chemical Biology, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, P.O. Box 80082, 3508 TB Utrecht, The Netherlands.
authors: Francesca
authors: F
authors: Pertici
authors: Norbert
authors: N
authors: Varga
authors: Arnoud
authors: A
authors: van Duijn
authors: Matias
authors: M
authors: Rey-Carrizo
authors: Anna
authors: A
authors: Bernardi
authors: Roland J
authors: RJ
authors: Pieters
keywords: LecA inhibition; Sonogashira reaction; multivalent carbohydrates; phenylene ethynylene; rigid spacers
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