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A facile synthesis of 8-amino-3-oxoindolizidine derivatives as conformationally restricted ornithyl pseudodipeptides

Autor: I. Gomez‐Monterrey, J. R. Harto, Rosario González-Muñiz, M. T. Garcia‐Lopez, Maria Dominguez

Publikováno v: Tetrahedron Letters. 32:1089-1092

One pot procedure for the synthesis of 8-amino-3-oxoindolizidines from Zδ-protected ornithyl ketomethylene pseudodipeptide derivatives is described. This procedure, involving hydrogenolysis of the Z-group, intramolecular reductive amination and γ-l

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::678d1f2615c8be04d03436f9b8a19ec7
https://doi.org/10.1016/s0040-4039(00)74495-9

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Synthesis and inhibitory activities against enkephalin degrading aminopeptidase of H-Trp(Nps)-Lys-OMe analogues bearing chelating groups

Autor: M. L. De Ceballos, J.C. del Río, Rosario González-Muñiz, J. R. Harto, T. Mme Garcia-Lopez

Publikováno v: Archiv der Pharmazie. 325(12)

With the aim of increasing the inhibitory potency of the analgesic dipeptide H-Trp(Nps)-Lys-OMe against enkephalin-degrading aminopeptidases, the following derivatives bearing chelating groups at the N-terminus have been synthesized: Ac-Trp(Nps)-Lys-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::de8ba4f96ac093eb1e3d0c74e228315e
https://pubmed.ncbi.nlm.nih.gov/1489252

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Prolonged antinociceptive activity of pseudodipeptide analogues of Lys-Trp(Nps) and Trp(Nps)-Lys

Autor: A.E. Lopez, Rosario González-Muñiz, M.L. De Ceballos, I. Gomez‐Monterrey, J.C. del Río, J. R. Harto, A. Bravo, M. T. Garcia‐Lopez

Publikováno v: Digital.CSIC. Repositorio Institucional del CSIC
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Peptide bend susbstitution in the molecules of Lys-Trp(Nps) (LTN) and Trp-(Nps)Lys (TNL) by an aminomethylene and ketomethylene bond, respectively, afforded pseudodipeptides with analgesic activity. The new compounds LysΨ(CH2NH)-Trp(Nps)-OMe (LTNAM)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f586059ec0bfb3943761acddbb997a2e
http://hdl.handle.net/10261/62865

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A simple and versatile route to ketomethylene dipeptide analogs

Autor: M. Teresa García-López, J. R. Harto, Rosario González-Muñiz

Publikováno v: Tetrahedron Letters. 29:1577-1580

A facile and versatile procedure for the synthesis of ketomethylene dipeptides by using Nα-Z-amino acid halomethyl ketones and dimethyl malonate as starting materials is reported. By application of this method, alanyl and phenylalanyl derivatives co

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ef2de532a1cb4efad4fb9aec3df26c47
https://doi.org/10.1016/s0040-4039(00)80357-3

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Synthesis of ketomethylene dipeptides containing basic amino acid analogues at c-terminus

Autor: Rosario González-Mufliz, María Teresa García-López, J. R. Harto

Publikováno v: Tetrahedron. 44:5131-5138

The four ketomethylene dipeptides Phe ψ(COCH2)( RS )Orn (6a) and Trp ψ(COCH2)( RS )X X=( RS )Orn (6b), ( RS )Arg (8b) and ( RS )Lys (12b) have been aynthasized by a route involving two successive principal reactions : a malonic ester alkylation wit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::35994d1d39d6c87f76bbf58b3e82a2fb
https://doi.org/10.1016/s0040-4020(01)86018-x

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Analgesic Dipeptides VI.: Synthesis and Structure-Activity Relationships of N-Terminal Modified Analogues of the Analgesic Compounds H-Xaa-Trp (Nps)-OMe (Xaa=Lys, Orn, Arg)

Autor: J. R. Harto, Rosario González-Muñiz, M. Teresa García-López, Joaquín Del Río, M. Teresa Molinero

Publikováno v: Archiv der Pharmazie. 322:145-152

In order to determine the influence of the N-terminal amino group of the dipeptide derivatives H-Xaa-Trp [(Nps)-OMe]Xaa=Lys (2a), Orn (2b), Arg (2c) on their antinociceptive effects, the syntheses of their corresponding deaminated, acetylated and dim

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::de18d89baa7325e202bdfe0b8dffc216
https://doi.org/10.1002/ardp.19893220306

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