New tetrazole-based selective anandamide uptake inhibitors

Giorgio Ortar; Aniello Schiano Moriello; Maria Grazia Cascio; Luciano De Petrocellis; Alessia Ligresti; Enrico Morera; Marianna Nalli; Vincenzo Di Marzo

doi:10.1016/j.bmcl.2008.04.003

New tetrazole-based selective anandamide uptake inhibitors

Giorgio Ortar^*, Aniello Schiano Moriello, Maria Grazia Cascio, Luciano De Petrocellis, Alessia Ligresti, Enrico Morera, Marianna Nalli, Vincenzo Di Marzo

^*Corresponding author for this work

Medical Sciences

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

32 Citations (Scopus)

Abstract

A new series of 1,5- and 2,5-disubstituted tetrazoles have been synthesized and evaluated as inhibitors of anandamide cellular uptake. Some of them inhibit the uptake process with a relatively high potency (IC₅₀ = 2.3-5.1 μM) and selectively over other proteins involved in endocannabinoid action and metabolism.

Original language	English
Pages (from-to)	2820-2824
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	9
DOIs	https://doi.org/10.1016/j.bmcl.2008.04.003
Publication status	Published - 1 May 2008

Keywords

Anandamide uptake
Anandamide uptake inhibitors
Endocannabinoids
Tetrazoles

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10.1016/j.bmcl.2008.04.003

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keywords = "Anandamide uptake, Anandamide uptake inhibitors, Endocannabinoids, Tetrazoles",

author = "Giorgio Ortar and {Schiano Moriello}, Aniello and Cascio, {Maria Grazia} and {De Petrocellis}, Luciano and Alessia Ligresti and Enrico Morera and Marianna Nalli and {Di Marzo}, Vincenzo",

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AU - Ortar, Giorgio

AU - Schiano Moriello, Aniello

AU - Cascio, Maria Grazia

AU - De Petrocellis, Luciano

AU - Ligresti, Alessia

AU - Morera, Enrico

AU - Nalli, Marianna

AU - Di Marzo, Vincenzo

PY - 2008/5/1

Y1 - 2008/5/1

N2 - A new series of 1,5- and 2,5-disubstituted tetrazoles have been synthesized and evaluated as inhibitors of anandamide cellular uptake. Some of them inhibit the uptake process with a relatively high potency (IC50 = 2.3-5.1 μM) and selectively over other proteins involved in endocannabinoid action and metabolism.

AB - A new series of 1,5- and 2,5-disubstituted tetrazoles have been synthesized and evaluated as inhibitors of anandamide cellular uptake. Some of them inhibit the uptake process with a relatively high potency (IC50 = 2.3-5.1 μM) and selectively over other proteins involved in endocannabinoid action and metabolism.

KW - Anandamide uptake

KW - Anandamide uptake inhibitors

KW - Endocannabinoids

KW - Tetrazoles

UR - http://www.scopus.com/inward/record.url?scp=42949106606&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2008.04.003

DO - 10.1016/j.bmcl.2008.04.003

M3 - Article

C2 - 18424134

AN - SCOPUS:42949106606

SN - 0960-894X

VL - 18

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EP - 2824

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 9

ER -

New tetrazole-based selective anandamide uptake inhibitors

Abstract

Keywords

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