Pyrazolo[3,4-d]pyrimidines as sigma-1 receptor ligands for the treatment of pain. Part 2: Introduction of cyclic substituents in position 4-Reference-Cited by-同舟云学术

Pyrazolo[3,4-d]pyrimidines as sigma-1 receptor ligands for the treatment of pain. Part 2: Introduction of cyclic substituents in position 4

Published:2017 Issue:6 Volume:8 Page:1246-1254
ISSN:2040-2503
Container-title:MedChemComm
language:en
Short-container-title:Med. Chem. Commun.

Author:

Díaz José Luis¹²³^ORCID,Corbera Jordi¹²³,Martínez Daniel¹²³^ORCID,Bordas Magda¹²³,Sicre Cristina⁴³,Pascual Rosalia¹²³,Pretel Mª José¹²³,Marín Ana Paz¹²³^ORCID,Montero Ana¹²³^ORCID,Dordal Albert¹²³^ORCID,Alvarez Inés¹²³^ORCID,Almansa Carmen¹²³^ORCID

Affiliation:

1. Drug Discovery and Preclinical Development

2. 08028 Barcelona

3. Spain

4. Galchimia

Abstract

A SAR study identified the 4-(1-methylpyrazol-5-yl) derivative, 12f, as a selective σ₁R antagonist with a good ADMET profile and potent antinociception.

Publisher

Royal Society of Chemistry (RSC)

Subject

Pharmaceutical Science,Biochemistry,Drug Discovery,Molecular Medicine,Pharmacology,Organic Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2017/MD/C7MD00078B

Reference24 articles.

1. A proposal for the classification of sigma binding sites

2. D. Zamanillo , E.Portillo-Salido , J. M.Vela and L.Romero , in Therapeutic Targets. Modulation, Inhibition and Activation , ed. J. M. Botana and M. Loza , John Wiley & Sons, Inc. , Hoboken, NJ , 2012 , pp. 225–278

3. Sigma-1 Receptor Chaperones at the ER- Mitochondrion Interface Regulate Ca2+ Signaling and Cell Survival

4. Sigma 1 receptor: A new therapeutic target for pain

5. Selective sigma-1 receptor antagonists for the treatment of pain

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