Synthesis and Binding Affinities of Novel SRIF-Mimicking β-<scp>d</scp>-Glucosides Satisfying the Requirement for a π-Cloud at C1

Ar, Angeles; Neagu, Irina; Et, Birzin; Er, Thornton; Smith, Andrew T.; Hirschmann, Ralph

doi:10.1021/ol050119i

Cited by 14 publications

(15 citation statements)

References 21 publications

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“…In fact it has been shown that properly functionalised β D-glucose scaffold can bind diverse GPCRs [35][36][37][38][39][40][41][42] and modulation of receptor and receptor subtype affinities can be achieved using diastereomeric and enantiomeric monosaccharide scaffolds as a means to structural and biological diversity. In fact it has been shown that properly functionalised β D-glucose scaffold can bind diverse GPCRs [35][36][37][38][39][40][41][42] and modulation of receptor and receptor subtype affinities can be achieved using diastereomeric and enantiomeric monosaccharide scaffolds as a means to structural and biological diversity.…”

Section: Privileged Structures Able To Interact With More Than a Givementioning

confidence: 99%

Bacterial Symbionts: Prospects for the Sustainable Production of Invertebrate-Derived Pharmaceuticals

Piel

2006

CMC

167

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Among the strategies that can lead to the discovery of new drugs, the identification and use of privileged structures, molecular fragments that are able to interact with more than one target, gained particular attention, in an attempt to find new drugs in a shorter time with respect to other strategies. These structures, that have been identified mainly by empirical observations, can target only a given protein family, or can be able to interact with more, unrelated targets. This review deals with structures not covered in recent papers on this topic, and emphasizes the importance of understanding the structure-target relationships, that confer the privileged status.

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Section: Privileged Structures Able To Interact With More Than a Givementioning

confidence: 99%

Bacterial Symbionts: Prospects for the Sustainable Production of Invertebrate-Derived Pharmaceuticals

Piel

2006

CMC

167

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Section: Privileged Structures Able To Interact With More Than a Givementioning

confidence: 99%

Privileged Structures as Leads in Medicinal Chemistry

Costantino¹,

Barlocco

2006

CMC

318

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The sol-gel process is an inorganic polymerization process taking place in mild conditions, allowing the association of mineral phases with organic or biological systems. The possibility to immobilize drugs, enzymes, antibodies and even whole cells without loss of their biological activity led to the development of diagnostic tools, drug delivery carriers as well as new hosts for artificial organ design. These systems take profit from the wide variety of chemical compositions, dimensions and forms that can be achieved via sol-gel chemistry. Recent advances involve multi-functional "smart" devices combining biocompatibility, biological activity and stimuli-responsive materials. The design of such novel devices with significant added value when compared to current products is probably a key factor when foreseeing industrial developments of sol-gel materials in medicinal science.

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“…Thioureas bearing an 3-(imidazol-4-yl)propyl group have dramatically reduced basicity in comparison with the -NH 2 group of Lys 9 of SRIF (pKa values of the side chain imidazole is about 7, whereas the -NH 2 group of Lys is about 10.5). Hirschmann [31,32] used electrostatic potential calculations to demonstrate that ben-zene, but not pyridine, could replace the indole ring in a series of glycoside-derived SRIF peptidomimetics. A recent report by Isaacs et al [30] on thrombin inhibitors showed that weakly basic imidazoles can function as surrogates for more basic alkylamines.…”

Section: Nonpeptide Ligands At Sstmentioning

confidence: 99%