59207-24-8Relevant articles and documents
Design and synthesis of piperazinylpyridine derivatives as novel 5-HT 1A agonists/5-HT3 antagonists for the treatment of irritable bowel syndrome (IBS)
Asagarasu, Akira,Matsui, Teruaki,Hayashi, Hiroyuki,Tamaoki, Satoru,Yamauchi, Yukinao,Sato, Michitaka
experimental part, p. 34 - 42 (2009/07/18)
We have prepared a series of piperazinylpyridine derivatives for the treatment of irritable bowel syndrome (IBS). These compounds, which were designed by pharmacophore analysis, bind to both serotonin subtype 1A (5-HT 1A) and subtype 3 (5-HT3) receptors. The nitrogen atom of the isoquinoline, a methoxy group and piper-azine were essential to the pharmacophore for binding to these receptors. We also synthesized furo- and thienopyridine derivatives according to structure-activity relationship analyses. Compound 17c (TZB-20810) had high affinities to these receptors and exhibited 5-HT1A agonistic activity and 5-HT3 antagonistic activity concurrently, and is a promising drug for further development in the treatment of IBS.
1-SUBSTITUTED AMINO-3-THIENO-[3,2-c]PYRIDINYLOXY-2-PROPANOLS
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, (2008/06/13)
This invention provides new compounds of formula I, STR1 wherein X is sulphur or oxygen,R is alkyl of 3 to 7 carbon atoms or cycloalkyl of 3 to 7 carbon atoms, cycloalkyl of 3 to 7 carbon atoms monosubstituted by alkyl of 1 to 4 carbon atoms, α-dialkylpropinyl of 5 to 9 carbon atoms or α-dialkyl-allyl of 5 to 9 carbon atoms, hydroxyalkyl of 2 to 7 carbon atoms or phenoxyalkyl of 8 to 11 carbon atoms, the oxygen atom of the last two radicals being separated by at least two carbon atoms from the nitrogen atom to which R is bound, R 1 isI. hydrogen or alkyl of 1 to 4 carbon atoms in the 2,3,6 or 7 position, orIi. chlorine or bromine, in the 2, 3 or 7 position,Iii. nitro or--NHA wherein A is alkanoyl of 1 to 4 carbon atoms, in the 2, 3 or 7 position, orIv. fluorine, cyano or COOB, wherein B is alkyl of 1 to 4 carbon atoms, in the 2 or 3 position, andR 2 isI. hydrogen or alkyl of 1 to 4 carbon atoms in the 2, 3, 6 or 7 position,Ii. chlorine or bromine, in the 2, 3 or 7 position, orIii. fluorine in the 2 or 3 position,Useful in the treatment of heart diseases.