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001-es BibID:	BIBFORM011369
Első szerző:	Herm, Laura
Cím:	N-Substituted-2-alkyl- and 2-arylnorapomorphines : Novel, highly active D2 agonists / Laura Herm, Sándor Berényi, Argo Vonk, Ago Rinken, Attila Sipos
Dátum:	2009
Megjegyzések:	Two synthesis routes have been elaborated for the preparation of novel N-substituted-2-alkyl- and 2-arylnorapomorphines. The first one utilizes the traditional methodology of N-substitution of morphinans before acid-catalyzed rearrangements into aporphinoids, while our new approach involves the N-substitution directly on the aporphine backbone. The aimed compounds were obtained in similar overall yields in different synthesis routes and were investigated with respect to their binding affinities and activities to dopamine D2 and D1 receptors. These studies revealed remarkable affinity and selectivity of some compounds for D2 over D1 receptor subtypes. Partial or full agonist properties were confirmed for all tested compounds.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban Apomorphine derivatives Suzuki-Miyaura reaction N-Substitution N-Oxidation Dopamine receptor activity
Megjelenés:	Bioorganic and Medicinal Chemistry. - 17 : 13 (2009), p. 4756-4762. -
További szerzők:	Berényi Sándor (1947-2019) (szerves kémikus) Vonk, Argo Rinken, Ago Sipos Attila (1977-) (vegyész, angol-magyar szakfordító)
Internet cím:	DOI Intézményi repozitóriumban (DEA) tárolt változat
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001-es BibID:	BIBFORM017684
Első szerző:	Reinart, Reet
Cím:	New 2-thioether-substituted apomorphines as potent and selective dopamine D2 receptor agonists / Reet Reinart, Zsuzsanna Gyulai, Sándor Berényi, Sándor Antus, Argo Vonk, Ago Rinken, Attila Sipos
Dátum:	2011
Megjegyzések:	A set of novel apomorphine derivatives were synthesized with diversely functionalized side chains in the proximity of position 2 of the aporphine skeleton. Amino and/or carboxylic functions were introduced to this region of the backbone to test their pharmacological effects. During the synthesis of 2-(S-3-mercaptopropionic acid)-derivative a heteroring-fused congener was also isolated. The structural elucidation confirmed that the formation of this product was in accordance with our previous observations on the reaction of thebaine (2) with thiosalycilic acid. All the novel apomorphine congeners 4aeg were neuropharmacologically characterized to discover their dopaminergic profiles. Two derivatives were identified as D2 full agonists equipotent with apomorphine (1) having significantly increased D2/D1 selectivity ratios.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban Apomorphine derivatives Parkinson's disease Structure-activity relationship Dopamine receptor activity Subtype selectivity
Megjelenés:	European Journal of Medicinal Chemistry. - 46 : 7 (2011), p. 2992-2999. -
További szerzők:	Gyulai Zsuzsanna Berényi Sándor (1947-2019) (szerves kémikus) Antus Sándor (1944-2022) (vegyészmérnök) Vonk, Argo Rinken, Ago Sipos Attila (1977-) (vegyész, angol-magyar szakfordító)
Pályázati támogatás:	K81701 OTKA
Internet cím:	DOI Intézményi repozitóriumban (DEA) tárolt változat
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