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- W207687690 endingPage "314" @default.
- W207687690 startingPage "243" @default.
- W207687690 abstract "The uses of 1,2,4-oxadiazoles include those as agonists at muscarinic receptors, 5-hydroxytryptamine (5-HT) receptor antagonists, benzodiazepine receptor agonists, potent antagonists of the (serotonin) 5-HT1B/D receptors, muscarinic receptor ‘superagonists’, selective inhibitors of human neutrophil elastase, and as active and selective A2B adenosine receptor antagonists. Much interest stems from the use of the fully conjugated 1,2,4-oxadiazole as a hydrolysis resistant ester or amide bioisostere and peptidomimetic. Amongst the non- fully conjugated systems, the soluble guanylyl cyclase inhibitor ODQ is a potent and selective inhibitor of nitric oxide-sensitive guanylyl cyclase and (S)-quisqualic acid is a neuroexcitatory naturally occurring amino acid. Synthetic approaches to the fully conjugated system are dominated by the conversion of a carboxylic acid into an activated derivative, followed by O-acylation of an amidoxime fragment and ring closure. A second popular route is 1,3-dipolar cycloaddition of a nitrile oxide to a nitrile. The reaction of an amidoxime with a carbonyl or the 1,3-dipolar cycloaddition of a nitrile oxide to an imine, or of a nitrone to a nitrile, provides the major routes to the nonconjugated dihydro-1,2,4-oxadiazoles. The reactions of fully conjugated 1,2,4-oxadiazoles and their nonconjugated analogues are detailed together with an in-depth analysis of their structural, theoretical, and thermodynamic properties." @default.
- W207687690 created "2016-06-24" @default.
- W207687690 creator A5018399098 @default.
- W207687690 date "2008-01-01" @default.
- W207687690 modified "2023-09-23" @default.
- W207687690 title "1,2,4-Oxadiazoles" @default.
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