Výsledky vyhledávání

Synthesis and Structure−Activity Relationships of a New Model of Arylpiperazines. 5. Study of the Physicochemical Influence of the Pharmacophore on 5-HT1A/α1-Adrenergic Receptor Affinity: Synthesis of a New Derivative with Mixed 5-HT1A/D2 Antagonist Properties

Autor: María L. López-Rodríguez, M. José Morcillo, Ma Eugenia Beneytez, Esther Fernandez, and Jorge Manzanares, L Orensanz, Esther Porras, Jose Angel Fuentes

Publikováno v: Journal of Medicinal Chemistry. 44:186-197

In this paper we have designed and synthesized a test series of 32 amide arylpiperazine derivatives VI in order to gain insight into the physicochemical influence of the pharmacophores of 5-HT1A and α1-adrenergic receptors. The training set was desi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e6d3ccd5823a07405c50066e81a97927
https://doi.org/10.1021/jm000929u

Zobrazit plný text záznamu

Synthesis and Structure−Activity Relationships of a New Model of Arylpiperazines. 3. 2-[ω-(4-Arylpiperazin-1-yl)alkyl]perhydropyrrolo- [1,2-c]imidazoles and -perhydroimidazo[1,5-a]pyridines: Study of the Influence of the Terminal Amide Fragment on 5-HT1A Affinity/Selectivity

Autor: María L. López-Rodríguez, A M Sanz, M. J. Morcillo, M Murcia, Esther Porras, L Orensanz, Esther Fernandez

Publikováno v: Journal of Medicinal Chemistry. 40:2653-2656

A series of new arylpiperazine derivatives 2, which are devoid of the terminal amide fragment present in related 5-HT1A ligands, was prepared and evaluated for affinity at 5-HT1A and alpha 1 receptors. All the compounds 2 demonstrated high affinity f

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::371928fe12ea115a2cfe2e20ffc56398
https://doi.org/10.1021/jm970216k

Zobrazit plný text záznamu

ALPHA.1-Adrenoceptor Reagents. Synthesis of Some 5,6,11,11a-Tetrahydro-1H-imidazo(1',5':1,6)pyrido and 5,6,11,11b-Tetrahydro-1H-imidazo(1',5':1,2)pyrido(3,4-b)indole-1,3(2H)-diones

Autor: María L. López-Rodríguez, Jorge Serrano, Esther Fernandez, Bellinda Benhamú, M. José Morcillo, L Orensanz

Publikováno v: Chemical and Pharmaceutical Bulletin. 43:941-946

Several 2-substituted 5,6,11,11a-tetrahydro-1H-imidazo[1',5':1,6]pyrido (1) and 5,6,11,11b-tetrahydro-1H-imidazo [1',5':1,2]pyrido[3,4-b]indole,3(2H)-diones (2) were synthesized and studied by 2D-NMR spectroscopy and difference nuclear Overhauser eff

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf861e3dd343686381b3a532e2e1ca8f
https://doi.org/10.1248/cpb.43.941

Zobrazit plný text záznamu

Reaction of 6-Hydroxytetrahydro-.BETA.-carboline-3-carboxylic Acids with Isocyanates and Isothiocyanates

Autor: Maria L. Lopez Rodriguez, Esther Fernandez, Mercedes López-Cuervo Garrido, Bellinda Benhamú, Fernando Benito, M. José Morcillo, L Orensanz

Publikováno v: Chemical and Pharmaceutical Bulletin. 42:2108-2112

The reaction of (-)-(3,S)-6-hydroxy-1,2,3,4-tetrahydro-beta-carboline-3-carboxylic acid (3a) with isocyanates and isothiocyanates gave the (+/-)-beta-carboline-hydantoin (4a-d) and -thiohydantoin systems (5a-d). The treatment of (-)-(1S,3S)-6-hydroxy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4fb8600ba9f93fc9ecaf290a18f1ee0f
https://doi.org/10.1248/cpb.42.2108

Zobrazit plný text záznamu

Study of plasma antioxidant status in Alzheimer's disease

Autor: R. Pulido, A. Jimenez-Escrig, L. Orensanz, F. Saura-Calixto

Publikováno v: Digital.CSIC. Repositorio Institucional del CSIC
instname

To examine the plasma antioxidant status of Alzheimer's disease (AD) patients and to evaluate the influence of apolipoprotein E (APOE) genotype. There are reasons to suspect involvement of the free hydroxyl radical in the pathogenesis of AD. In contr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c57cf354cf1a090608b1825bea1fef2
http://hdl.handle.net/10261/122024

Zobrazit plný text záznamu

Synthesis and structure-activity relationships of a new model of arylpiperazines. 5. Study of the physicochemical influence of the pharmacophore on 5-HT(1a)/alpha(1)-adrenergic receptor affinity: synthesis of a new derivative with mixed 5-HT(1a)/d(2) antagonist properties

Autor: M L, López-Rodríguez, M J, Morcillo, E, Fernández, E, Porras, L, Orensanz, M E, Beneytez, J, Manzanares, J A, Fuentes

Publikováno v: Journal of medicinal chemistry. 44(2)

In this paper we have designed and synthesized a test series of 32 amide arylpiperazine derivatives VI in order to gain insight into the physicochemical influence of the pharmacophores of 5-HT(1A) and alpha(1)-adrenergic receptors. The training set w

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::883cc4eff0b4d3586b8c9366a193bf62
https://pubmed.ncbi.nlm.nih.gov/11170628

Zobrazit plný text záznamu

Benzimidazole derivatives. 2. Synthesis and structure-activity relationships of new azabicyclic benzimidazole-4-carboxylic acid derivatives with affinity for serotoninergic 5-HT(3) receptors

Autor: Bellinda Benhamú, L Orensanz, Tejada Id, María L. López-Rodríguez, Alfaro Mj, Martín Mi, M. J. Morcillo

Publikováno v: Journal of medicinal chemistry. 42(24)

A new series of azabicyclic benzimidazole-4-carboxamides 2-21 and -carboxylates 22-30 were synthesized and evaluated for binding affinity at serotoninergic 5-HT(3) and 5-HT(4) receptors in the CNS. Most of the synthesized compounds exhibited high or

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a6370b77d18166781514016ef8a6eab2
https://pubmed.ncbi.nlm.nih.gov/10585211

Zobrazit plný text záznamu

Design and synthesis of 2-[4-[4-(m-(ethylsulfonamido)-phenyl) piperazin-1-yl]butyl]-1,3-dioxoperhydropyrrolo[1,2-c]imidazole (EF-7412) using neural networks. A selective derivative with mixed 5-HT1A/D2 antagonist properties

Autor: M L, López-Rodríguez, M J, Morcillo, E, Fernández, M L, Rosado, L, Orensanz, M E, Beneytez, J, Manzanares, J A, Fuentes, K J, Schaper

Publikováno v: Bioorganicmedicinal chemistry letters. 9(12)

A test series of 32 phenylpiperazines III with affinity for 5-HT1A and alpha1 receptors was subjected to QSAR analysis using artificial neural networks (ANNs), in order to get insight into the structural requirements that are responsible for 5-HT1A/a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::41f37d40cf865b238096b65ea53e86da
https://pubmed.ncbi.nlm.nih.gov/10397500

Zobrazit plný text záznamu

Transthyretin Tyr77 familial amyloid polyneuropathy: a clinicopathological study of a large kindred

Autor: C R, Blanco-Jerez, A, Jiménez-Escrig, J M, Gobernado, S, Lopez-Calvo, G, de Blas, C, Redondo, M, García Villanueva, L, Orensanz

Publikováno v: Musclenerve. 21(11)

More than 40 point mutations (producing different clinical manifestations) have been described in diverse points of the plasma protein transthyretin (TTR). The Met30 is considered the most common mutation, the Tyr77 mutation being the second most pre

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::79b67341a9ebe7948d137fb3cb14c5f1
https://pubmed.ncbi.nlm.nih.gov/9771673

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání