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Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse

A series of 3,6-disubstituted β-carbolines was synthesized and evaluated for their in vitro affinities at α β γ GABA /benzodiazepine receptor subtypes by radioligand binding assays in search of α subtype selective ligands to treat alcohol abuse. Analogues of β-carboline-3-carboxylate- -butyl ester (... Full description

Journal Title: Bioorganic & Medicinal Chemistry 2010, Vol.18(21), pp.7548-7564
Main Author: Yin, Wenyuan
Other Authors: Majumder, Samarpan , Clayton, Terry , Petrou, Steven , Vanlinn, Michael L , Namjoshi, Ojas A , Ma, Chunrong , Cromer, Brett A , Roth, Bryan L , Platt, Donna M , Cook, James M
Format: Electronic Article Electronic Article
Language: English
Subjects:
ID: ISSN: 0968-0896 ; E-ISSN: 1464-3391 ; DOI: 10.1016/j.bmc.2010.08.049
Link: https://www.sciencedirect.com/science/article/pii/S0968089610008059
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recordid: elsevier_sdoi_10_1016_j_bmc_2010_08_049
title: Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse
format: Article
creator:
  • Yin, Wenyuan
  • Majumder, Samarpan
  • Clayton, Terry
  • Petrou, Steven
  • Vanlinn, Michael L
  • Namjoshi, Ojas A
  • Ma, Chunrong
  • Cromer, Brett A
  • Roth, Bryan L
  • Platt, Donna M
  • Cook, James M
subjects:
  • Beta-Carboline
  • Benzodiazepine
  • Alcohol Antagonist
  • Gaba Receptor
  • Medicine
  • Chemistry
  • Anatomy & Physiology
ispartof: Bioorganic & Medicinal Chemistry, 2010, Vol.18(21), pp.7548-7564
description: A series of 3,6-disubstituted β-carbolines was synthesized and evaluated for their in vitro affinities at α β γ GABA /benzodiazepine receptor subtypes by radioligand binding assays in search of α subtype selective ligands to treat alcohol abuse. Analogues of β-carboline-3-carboxylate- -butyl ester (βCCt, ) were synthesized via a CDI-mediated process and the related 6-substituted β-carboline-3-carboxylates including WYS8 ( ) were synthesized via a Sonogashira or Stille coupling processes from 6-iodo-βCCt ( ). The bivalent ligands of βCCt ( and ) were also designed and prepared via a palladium-catalyzed homocoupling process to expand the structure–activity relationships (SAR) to larger ligands. Based...
language: eng
source:
identifier: ISSN: 0968-0896 ; E-ISSN: 1464-3391 ; DOI: 10.1016/j.bmc.2010.08.049
fulltext: fulltext
issn:
  • 0968-0896
  • 09680896
  • 1464-3391
  • 14643391
url: Link


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titleDesign, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse
creatorYin, Wenyuan ; Majumder, Samarpan ; Clayton, Terry ; Petrou, Steven ; Vanlinn, Michael L ; Namjoshi, Ojas A ; Ma, Chunrong ; Cromer, Brett A ; Roth, Bryan L ; Platt, Donna M ; Cook, James M
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descriptionA series of 3,6-disubstituted β-carbolines was synthesized and evaluated for their in vitro affinities at α β γ GABA /benzodiazepine receptor subtypes by radioligand binding assays in search of α subtype selective ligands to treat alcohol abuse. Analogues of β-carboline-3-carboxylate- -butyl ester (βCCt, ) were synthesized via a CDI-mediated process and the related 6-substituted β-carboline-3-carboxylates including WYS8 ( ) were synthesized via a Sonogashira or Stille coupling processes from 6-iodo-βCCt ( ). The bivalent ligands of βCCt ( and ) were also designed and prepared via a palladium-catalyzed homocoupling process to expand the structure–activity relationships (SAR) to larger ligands. Based...
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