Literature DB >> 15975799

Insight into 2-phenylpyrazolo[1,5-a]pyrimidin-3-yl acetamides as peripheral benzodiazepine receptor ligands: synthesis, biological evaluation and 3D-QSAR investigation.

Silvia Selleri1, Paola Gratteri, Camilla Costagli, Claudia Bonaccini, Annarella Costanzo, Fabrizio Melani, Gabriella Guerrini, Giovanna Ciciani, Barbara Costa, Francesca Spinetti, Claudia Martini, Fabrizio Bruni.   

Abstract

The present paper reports the synthesis and binding studies of new 2-phenylpyrazolo[1,5-a]pyrimidin-3-yl acetamides as selective Peripheral Benzodiazepine Receptor (PBR) ligands. The variability of substituents at the 3-position was investigated and a 3D-QSAR model was proposed to evaluate the effect of different substitutions on the acetamide moiety. In addition, a subset of the novel compounds showing high affinity for PBR was tested for their ability to modulate the steroid biosynthesis in C6 glioma cells.

Entities:  

Mesh:

Substances:

Year:  2005        PMID: 15975799     DOI: 10.1016/j.bmc.2005.05.015

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  7 in total

1.  New structure-activity relationships of N-acetamide substituted pyrazolopyrimidines as pharmacological ligands of TSPO.

Authors:  Jun Li; Michael L Schulte; Michael L Nickels; H Charles Manning
Journal:  Bioorg Med Chem Lett       Date:  2016-06-16       Impact factor: 2.823

2.  Mixed-affinity binding in humans with 18-kDa translocator protein ligands.

Authors:  David R J Owen; Roger N Gunn; Eugenii A Rabiner; Idriss Bennacef; Masahiro Fujita; William C Kreisl; Robert B Innis; Victor W Pike; Richard Reynolds; Paul M Matthews; Christine A Parker
Journal:  J Nucl Med       Date:  2010-12-13       Impact factor: 10.057

3.  N-(2-Bromo-4-methyl-phen-yl)-2-(5-methyl-2-phenyl-pyrazolo-[1,5-a]pyrimidin-7-yl)acetamide.

Authors:  Ibtissam Bassoude; Sabine Berteina-Raboin; El Mokhtar Essassi; Gérald Guillaumet; Lahcen El Ammari
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-05-04

4.  Approaches towards the synthesis of 5-aminopyrazoles.

Authors:  Ranjana Aggarwal; Vinod Kumar; Rajiv Kumar; Shiv P Singh
Journal:  Beilstein J Org Chem       Date:  2011-02-09       Impact factor: 2.883

5.  Novel Derivatives of diphenyl-1,3,4-oxadiazol as Ligands of Benzodiazepine Receptors; Synthesize, Binding Assay and Pharmacological Evaluation.

Authors:  Mona Khoramjouy; Naeime Zarepishe; Elham Rezaee; Ali Imani; Rojin Mahmoudzadeh-Mandolakani; Seyedali Hashemi; Moones Fallah; Golnar Hasheminasab; Soraya Shahhosseini; Sayyed Abbas Tabatabai; Mehrdad Faizi
Journal:  Iran J Pharm Res       Date:  2021       Impact factor: 1.696

6.  7-Chloro-5-methyl-2-phenyl-pyrazolo-[1,5-a]pyrimidine.

Authors:  Ibtissam Bassoude; Sabine Berteina-Raboin; El Mokhtar Essassi; Gérald Guillaumet; Lahcen El Ammari
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-04-17

7.  Ethyl 7-methyl-2-phenyl-pyrazolo-[1,5-a]pyrimidine-5-carboxyl-ate.

Authors:  Ibtissam Bassoude; Sabine Berteina-Raboin; El Mokhtar Essassi; Gérald Guillaumet; Lahcen El Ammari
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-04-17
  7 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.