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A series of analogues of the non-steroidal anti-inflammatory drug (NSAID) sulindac 1 were synthesised tethered to nitric oxide (NO) donating functional groups. Sulindac shows antiproliterative… (More)
Functionalised azepane and oxepane scaffolds were prepared using diazocarbonyl chemistry and elaborated to show their potential use in library synthesis. Key dicarbonyl containing seven-membered… (More)
Flash vacuum pyrolysis (FVP) at 500–600 °C of 1-substituted pyrazolylaminomethylene derivatives of Meldrum’s acid provides 1-substituted pyrazolo[3,4- b ]pyridin-4-ones in high yields. If the… (More)
Analogues of the nicotinic acetylcholine antagonist epibatidine, suitable for diversification, were synthesized by application of a pyrrole Diels–Alder strategy, allowing rapid generation of… (More)
Functionalised tetrahydropyran scaffolds were prepared using a tethered enol-ether Prins cyclisation and elaborated to show their potential use in library synthesis. The key 4-hydroxytetrahydropyran… (More)
The synthesis of four novel amino acids carrying nitric oxide-releasing motifs is presented (protected derivatives (VI), (VIII), and (X) are depicted).
The presented method has several advantages such as simple procedure, ease of isolation, good yields, and high tolerance of functional and protecting groups.
A new route to spiro-oxetanes, potential scaffolds for drug discovery, is described. The route is based on the selective 1,4-C-H insertion reactions of metallocarbenes, generated from simple carbonyl… (More)
1,2-Diazetidin-3-ones are readily accessible, small ring scaffolds that upon functionalization have the potential to produce diverse 3-dimensional structures for drug discovery. Thus, treatment of… (More)