Monocyclic analogues of the μ-opioid agonist 3,8-diazabicyclo [3.2.1]octanes: Synthesis, modeling, and activity

Daniela Barlocco; Stefania Villa; Walter Fratta; Paola Fadda; Diego Colombo; Lucio Toma

doi:10.1016/0040-4020(95)00716-L

Monocyclic analogues of the μ-opioid agonist 3,8-diazabicyclo [3.2.1]octanes: Synthesis, modeling, and activity

Daniela Barlocco, Stefania Villa, Walter Fratta, Paola Fadda, Diego Colombo, Lucio Toma

Fondazione IRCCS Ca' Granda- Ospedale Maggiore Policlinico

Research output: Contribution to journal › Article › peer-review

Abstract

Several monocyclic derivatives structurally related to the μ-opioid agonist 3-cinnamyl-8 propionyl-3,8-diazabicyclo[3.2. 1]octane have been synthesized and tested in binding studies using the μ-selective ³H-DAMGO as ligand. Modeling studies have been performed on the same compounds in order to explain the observed lack of affinity towards μ-opioid receptors.

Original language	English
Pages (from-to)	11547-11556
Number of pages	10
Journal	Tetrahedron
Volume	51
Issue number	42
DOIs	https://doi.org/10.1016/0040-4020(95)00716-L
Publication status	Published - Oct 16 1995

ASJC Scopus subject areas

Biochemistry
Organic Chemistry
Drug Discovery

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title = "Monocyclic analogues of the μ-opioid agonist 3,8-diazabicyclo [3.2.1]octanes: Synthesis, modeling, and activity",

abstract = "Several monocyclic derivatives structurally related to the μ-opioid agonist 3-cinnamyl-8 propionyl-3,8-diazabicyclo[3.2. 1]octane have been synthesized and tested in binding studies using the μ-selective 3H-DAMGO as ligand. Modeling studies have been performed on the same compounds in order to explain the observed lack of affinity towards μ-opioid receptors.",

author = "Daniela Barlocco and Stefania Villa and Walter Fratta and Paola Fadda and Diego Colombo and Lucio Toma",

year = "1995",

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doi = "10.1016/0040-4020(95)00716-L",

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T1 - Monocyclic analogues of the μ-opioid agonist 3,8-diazabicyclo [3.2.1]octanes

T2 - Synthesis, modeling, and activity

AU - Barlocco, Daniela

AU - Villa, Stefania

AU - Fratta, Walter

AU - Fadda, Paola

AU - Colombo, Diego

AU - Toma, Lucio

PY - 1995/10/16

Y1 - 1995/10/16

N2 - Several monocyclic derivatives structurally related to the μ-opioid agonist 3-cinnamyl-8 propionyl-3,8-diazabicyclo[3.2. 1]octane have been synthesized and tested in binding studies using the μ-selective 3H-DAMGO as ligand. Modeling studies have been performed on the same compounds in order to explain the observed lack of affinity towards μ-opioid receptors.

AB - Several monocyclic derivatives structurally related to the μ-opioid agonist 3-cinnamyl-8 propionyl-3,8-diazabicyclo[3.2. 1]octane have been synthesized and tested in binding studies using the μ-selective 3H-DAMGO as ligand. Modeling studies have been performed on the same compounds in order to explain the observed lack of affinity towards μ-opioid receptors.

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U2 - 10.1016/0040-4020(95)00716-L

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JO - Tetrahedron

JF - Tetrahedron

SN - 0040-4020

IS - 42

ER -

Monocyclic analogues of the μ-opioid agonist 3,8-diazabicyclo [3.2.1]octanes: Synthesis, modeling, and activity

Abstract

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