Výsledky vyhledávání - "Eudysmic ratio"

Pyrrolidine-based 3-deoxysphingosylphosphorylcholine analogs as possible candidates against neglected tropical diseases (NTDs): identification of hit compounds towards development of potential treatment of Leishmania donovani

Autor: Hye Rim Jeon, Trong-Nhat Phan, Ahmed H.E. Hassan, Seolmin Yoon, Yong Sup Lee, Cheol Jung Lee, Seung-Hwan Kim, Joo Hwan No

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry
article-version (VoR) Version of Record
Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 36, Iss 1, Pp 1922-1930 (2021)

A rational-based process was adopted for repurposing pyrrolidine-based 3-deoxysphingosylphosphorylcholine analogs bearing variable acyl chains, different stereochemical configuration and/or positional relationships. Structural features were highly in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0b19cb64eb265e2bfbe864c8accb7402
https://doi.org/10.1080/14756366.2021.1969385

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Chemoenzymatic synthesis of 2,6-disubstituted tetrahydropyrans with high σ1 receptor affinity, antitumor and analgesic activity

Autor: Nicole Kopp, Erik Laurini, Hans-Ulrich Humpf, Dirk Schepmann, Carmen Almansa, Francisco R. Nieto, Sabrina Pricl, Gianluca Civenni, Domenico Marson, Carlo V. Catapano, Bernhard Wünsch

1,3-Dioxanes 1 and cyclohexanes 2 bearing a phenyl ring and an aminoethyl moiety in 1,3-relationship to each other represent highly potent σ1 receptor antagonists. In order to increase the chemical stability of the acetalic 1,3-dioxanes 1 and the po

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7a1ecbc0b94c8f1e4352a2e829847b05
https://www.sciencedirect.com/science/article/pii/S0223523421002920?via=ihub

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Chiral Separation, X-ray Structure, and Biological Evaluation of a Potent and Reversible Dual Binding Site AChE Inhibitor

Autor: Israel Silman, Marco Catto, Rocco Caliandro, Jacques-Philippe Colletier, Giuseppe Felice Mangiatordi, Cosimo Altomare, Orazio Nicolotti, Nunzio Denora, Eugenio de la Mora, Annalisa De Palma, Andrea Pinto, Benny Danilo Belviso, Leonardo Pisani

Publikováno v: ACS Medicinal Chemistry Letters
ACS Medicinal Chemistry Letters, American Chemical Society, 2020, 11 (5), pp.869-876. ⟨10.1021/acsmedchemlett.9b00656⟩
ACS Medicinal Chemistry Letters, 2020, 11 (5), pp.869-876. ⟨10.1021/acsmedchemlett.9b00656⟩
ACS Med Chem Lett
ACS medicinal chemistry letters (2020). doi:10.1021/acsmedchemlett.9b00656
info:cnr-pdr/source/autori:Marco Catto 1, *, Leonardo Pisani 1, Eugenio de la Mora 2, Benny Danilo Belviso 3, Giuseppe Felice Mangiatordi 3, Andrea Pinto 4, Annalisa De Palma 5, Nunzio Denora 1, Rocco Caliandro 3, Jacques-Philippe Colletier 2, Israel Silman 6, Orazio Nicolotti 1, Cosimo Damiano Altomare 1/titolo:Chiral Separation, X-ray Structure, and Biological Evaluation of a Potent and Reversible Dual Binding Site AChE Inhibitor/doi:10.1021%2Facsmedchemlett.9b00656/rivista:ACS medicinal chemistry letters/anno:2020/pagina_da:/pagina_a:/intervallo_pagine:/volume

International audience; Acetylcholinesterase (AChE) inhibitors (AChEIs) still remain the leading therapeutic options for the symptomatic treatment of cognitive deficits associated with mild-to-moderate Alzheimer's disease. The search for new AChEIs b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::db51b18f24b39a006e1f258797dc8cae
https://hal.univ-grenoble-alpes.fr/hal-02864326

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Synthesis and Pharmacological Evaluation of Enantiomerically Pure GluN2B Selective NMDA Receptor Antagonists

Autor: Julian A. Schreiber, Thomas J. Schmidt, Louisa Temme, Marina Szermerski, Guiscard Seebohm, Simon M. Ametamey, Bernhard Wünsch, Dirk Schepmann, Nathalie Strutz-Seebohm, Kirstin Lehmkuhl, Frederik Börgel

Publikováno v: ChemMedChem. 13:1580-1587

To determine the eutomers of potent GluN2B-selective N-methyl-d-aspartate (NMDA) receptor antagonists with a 3-benzazepine scaffold, 7-benzyloxy-3-(4-phenylbutyl)-2,3,4,5-tetrahydro-1H-3-benzazepin-1-ols (S)-2 and (R)-2 were separated by chiral HPLC.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a939ab5ca52046364ee6fb0f46fc0525
https://doi.org/10.1002/cmdc.201800214

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Ethynylogation approach in pharmacophore design: from alkynyl-to butadiynyl-carbinols vs antitumoral cytotoxicity

Autor: Valérie Maraval, Yves Génisson, Remi Chauvin, Isabelle Fabing, Etienne Joly, Nathalie Saffon-Merceron, Dymytrii Listunov

Publikováno v: Tetrahedron
Tetrahedron, Elsevier, 2016, 72 (42), pp.6697-6704. ⟨10.1016/j.tet.2016.09.001⟩

International audience; Ethynylogation of a chiral lipidic dialkynylcarbinol (DAC), identified as a lead for cytotoxicity against HCT116 cancer cells, is shown to typify the butadiynyl-alkynylcarbinol (BAC) unit as a new pharmacophore. The enantiomer

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2a27cb9dbc9c7c7386fef07070c59ef5
https://doi.org/10.1016/j.tet.2016.09.001

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4-isoxazolyl-1,4-dihydropyridines: a tale of two scaffolds

Autor: Nicholas R. Natale, Scott A. Steiger

Publikováno v: Future Medicinal Chemistry. 6:923-943

The association of the isoxazole and dihydropyridine (DHP) ring systems fused at the 4'-isoxazolyl- to the 4-position of the DHP has produced a combination scaffold, the isoxazolyl-DHPs (IDHPs) with unique conformational characteristics. The IDHPs ar

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed26242e0340c1ebd52b3a752396433c
https://doi.org/10.4155/fmc.14.46

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Tetrahydro-naphthols as orally available TRPV1 inhibitors

Autor: Muneto Mogi, Yuka Ikegami, Klaus Urbahns, Masaomi Tajimi, Takeshi Yura, Marumo Makiko, David Madge, Noriyuki Yamamoto, Kayo Yasoshima, Tsutomu Masuda, Jang Bahadur Gupta, Nagahiro Yoshida, Fiona Chan, Hiroshi Fujishima, Toshiya Moriwaki

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:3408-3411

Starting from a naphthol-based lead series with low oral bioavailability, we have identified potent TRPV1 antagonists with oral bioavailability in rats. These compounds emerged from SAR studies aimed at replacing the lead's phenol structure whilst ma

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb33921a125c30096403ba92dfcdaac9
https://doi.org/10.1016/j.bmcl.2012.03.108

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Synthesis of enantiomerically pure HIP-A and HIP-B and investigation of their activity as inhibitors of excitatory amino acid transporters

Autor: Giovanni Grazioso, Carlo De Micheli, Lucia Tamborini, Andrea Pinto, Marco De Amici, Paola Conti, Simona Colleoni, Marco Gobbi, Tiziana Mennini

Publikováno v: Tetrahedron: Asymmetry. 19:867-875

The present report deals with the synthesis of the two couples of enantiomers (+)-(3aS,4R,6aS)-/(−)-(3aR,4S,6aR)-3-hydroxy-3a,4,6,6a-tetrahydro-pyrrolo[3,4-d]isoxazole-4-carboxylic acid [(+)-HIP-A and (−)-HIP-A] and (+)-(3aS,6S,6aS)-/(−)-(3aR,6

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::807080b26a16e92c599120aac3fcb4b8
https://doi.org/10.1016/j.tetasy.2008.03.001

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Imidazoline Binding Sites (IBS) Profile Modulation: Key Role of the Bridge in Determining I1-IBS or I2-IBS Selectivity within a Series of 2-Phenoxymethylimidazoline Analogues

Autor: Mario Giannella, Josiane Feldman, Francesco Gentili, Wilma Quaglia, Livio Brasili, Alessandro Piergentili, Francesca Ghelfi, Maria Pigini, Pascal Bousquet, Monique Dontenwill

Publikováno v: Journal of Medicinal Chemistry. 46:2169-2176

The α- and β-methyl derivatives of 2-phenylethylimidazoline (compounds 7 and 8) and the corresponding enantiomers were prepared and tested with the purpose of studying the role played by the ethylene bridge in modulating Ii- and I 2 -IBS selectivit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::774124dccf5fa849a50c50c8fb851fb8
https://doi.org/10.1021/jm021113r

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