Bifunctional Variations of the Antidepressant Amitriptyline Theme
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概要
- 論文の詳細を見る
In an attempt to inhibit uptake sites for biogenic amines, the following "rigid" and "flexible" bifunctional analogues of amitriptyline of various topologies have been synthesized and evaluated as antidepressants : 5,7-bis (3-dimethylaminopropylidene)-12,13,15,16-tetrahydrobisbenzo-cyclohepta [7,6-a ; 6', 7'-d] bezene (7), 5,13-bis (3-dimethylaminopropylidene)-7,8,15,16-tetrahy-drobisbenzocyclohepta [6,7-a ; 6', 7'-d] benzene (8), 9,18-bis (3-dimethylaminopropylidene)-4b, 4c, 13b, 13c-tetrahydrotetrabenzo [a, d, h, k] dicycloheptacyclobutene (9), and 1,2-bis [3,3'-(5-N, N-dimethylaminopropylidene [5H] dibenzo [a, d] cyclohepten)] ethane (12). All were active as measured by the uptake inhibition of ^3H-serotonin into human blood platelets. Their structure-activity relationships revealed somewhat lower activity as compared with amitriptyline (1) but indicated the bifunctional amitriptylines can still interact with the uptake site. The synthesis and molecular structures including stereochemistry of the chiral pentacyclic aminoalcohol precursors (R, R and S, S)-4 and (R, S)-5 are reported. Strong intramolecular O-H・・・N bonding in 4 and 5 are noted.
- 公益社団法人日本薬学会の論文
- 1985-11-25
著者
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Agranat Israel
Department Of Organic Chemistry The Hebrew University Of Jerusalem
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Lindley Peter
Department Of Crystallography Birckbeck College University Of London
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ASSCHER YAEL
Department of Organic Chemistry, The Hebrew University of Jerusalem
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ROTMAN AVNER
Department of Membrane Research, The Weizmann Institute of Science
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Rotman Avner
Department Of Membrane Research The Weizmann Institute Of Science
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Asscher Yael
Department Of Organic Chemistry The Hebrew University Of Jerusalem
関連論文
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