Publication
Synthesis and acetylcholinesterase/butyrylcholin-esterase inhibition activity of 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro(and thieno)[2,3-b]quinolines, and 4-amino-5,6,7,8,9-pentahydro-2,3-diphenylcyclohepta[e]furo(and thieno)-[2,3-b]pyridine
| dc.contributor.author | Marco, JL | |
| dc.contributor.author | de los Rios, C | |
| dc.contributor.author | Carreiras, MC | |
| dc.contributor.author | Banos, JE | |
| dc.contributor.author | Badia, A | |
| dc.contributor.author | Vivas, NM | |
| dc.date.accessioned | 2015-12-30T10:18:03Z | |
| dc.date.available | 2015-12-30T10:18:03Z | |
| dc.date.issued | 2002 | |
| dc.description.abstract | The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibition activities of a series of 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (10-12)/4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (14) and 4-amino-5,6,7,8,9-pentahydro-2,3-diphenylcyclohepta[e]furo[2,3-b]pyridine (13)/4amino-5,6,7,8,9-pentahydro-2,3-phenylcyclohepta[e]thieno[2,3-b]pyridine (15) are described. These compounds are tacrine (THA) analogues which have been prepared either from readily available 2-amino-3-cyano-4,5-diarylfurans (16-18) or from 2-amino-3-cyano-4,5-diphenylthiophene (19), via Friedlander condensation with cyclohexanone or cycloheptanone. These compounds are competitive inhibitors for acetylcholinesterase, the more potent being compound (13) which is threefold less active than tacrine. The butyrylcholinesterase inhibition activity is significant only in compounds 10 and 13, which are ten-fold less active than tacrine. It is found that the products 11 and 12 strongly inhibit acetylcholinesterase, and show excellent selectivity regarding butyrylcholinesterase. | |
| dc.format | application/pdf | |
| dc.identifier.citation | ARCHIV DER PHARMAZIE. - Vol. 335, n. 7 (JUL 2002), p. 347-353 | |
| dc.identifier.issn | 0365-6233 | |
| dc.identifier.uri | http://hdl.handle.net/10451/21380 | |
| dc.language.iso | eng | |
| dc.publisher | WILEY-V C H VERLAG GMBH | |
| dc.subject | Chemistry, Medicinal | |
| dc.subject | Chemistry, Multidisciplinary | |
| dc.subject | Pharmacology & Pharmacy | |
| dc.title | Synthesis and acetylcholinesterase/butyrylcholin-esterase inhibition activity of 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro(and thieno)[2,3-b]quinolines, and 4-amino-5,6,7,8,9-pentahydro-2,3-diphenylcyclohepta[e]furo(and thieno)-[2,3-b]pyridine | |
| dc.type | journal article | |
| dspace.entity.type | Publication | |
| oaire.citation.endPage | 353 | por |
| oaire.citation.startPage | 347 | por |
| oaire.citation.title | ARCHIV DER PHARMAZIE | por |
| oaire.citation.volume | Vol. 335 | por |
| rcaap.rights | restrictedAccess | |
| rcaap.type | article |