39891-55-9Relevant articles and documents
Development of an enolate alkynylation approach towards the synthesis of the taiwanschirin natural products
Christensen, Kirsten E.,Donohoe, Timothy J.,Haughey, Maxwell B.,Poole, Darren L.
, p. 13392 - 13397 (2021/11/01)
Through the use of model studies, an approach was conceived towards the synthesis of the taiwanschirin family of natural products. These are structurally complex compounds which represent highly challenging and biologically active targets for total synthesis. This work describes a successful synthesis of the complex taiwanschirin fused [8,6,5] core through a novel alkynylation reaction coupled with an intramolecular Heck reaction used to construct the 8-membered ring.
Modulators of the Cystic Fibrosis Transmembrane Conductance Regulator Protein and Methods of Use
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Paragraph 0967, (2018/09/16)
The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the inventi
Further structure-activity relationships in the series of tropanyl esters endowed with potent antinociceptive activity
Scapecchi, Serena,Giorgi, Antonella,Bellucci, Cristina,Dei, Silvia,Ghelardini, Carla,Manetti, Dina,Romanelli, M. Novella,Teodori, Elisabetta
, p. 764 - 772 (2007/10/03)
Several analogs of the α-tropanyl esters of 2-(4-chlorophenoxy)butyric acid (SM21) and 2-phenylthiobutyric acid (SM32), endowed with potent antinociceptive and cognition enhancing activity, were synthesized, aimed at obtaining more potent and safe drug candidates. Variation of the acyl moiety, as well as the conformational restriction of atropine to give the α-tropanyl ester of 2,3-dihydrobenzofurane-3-carboxylic acid (18), practically abolished activity. In the case of 18, the antimuscarinic activity was also severely affected by the conformation restrain. On the contrary, conformational restriction of phenoxybutyric and phenylthiobutyric acid derivatives to give the α-tropanyl ester of 2,3-dihydro-benzofurane-2-carboxylic acid and 2,3-dihydro-benzothiophene-2-carboxylic acid, afforded potent analgesic drugs that unfortunately were too toxic to be reliable drug candidates. A series of related esters of benzofurane-3-carboxylic acid and benzothiophene-3-carboxylic acid were also studied and found to be potent but toxic analgesics.