Literature DB >> 8388472

Structure-activity relationship studies at the benzodiazepine receptor (BZR): a comparison of the substitutent effects of pyrazoloquinolinone analogs.

R I Fryer1, P Zhang, R Rios, Z Q Gu, A S Basile, P Skolnick.   

Abstract

The synthesis of a series of 2-phenylpyrazolo[4,3-c]quinolin-3-one derivatives and their in vitro biological evaluation as ligands for the benzodiazepine receptor are described. The in vitro activities, as determined by an analysis of GABA shift ratios, and binding affinities of these compounds to BZR are compared in terms of the electronic, lipophilic, and steric effect changes of their substituents.

Entities:  

Mesh:

Substances:

Year:  1993        PMID: 8388472     DOI: 10.1021/jm00063a017

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  8 in total

1.  Discovery of Plasmodium vivax N-myristoyltransferase inhibitors: screening, synthesis, and structural characterization of their binding mode.

Authors:  Victor Goncalves; James A Brannigan; David Whalley; Keith H Ansell; Barbara Saxty; Anthony A Holder; Anthony J Wilkinson; Edward W Tate; Robin J Leatherbarrow
Journal:  J Med Chem       Date:  2012-04-03       Impact factor: 7.446

2.  Unexpected Properties of δ-Containing GABAA Receptors in Response to Ligands Interacting with the α+ β- Site.

Authors:  Pantea Mirheydari; Joachim Ramerstorfer; Zdravko Varagic; Petra Scholze; Laurin Wimmer; Marko M Mihovilovic; Werner Sieghart; Margot Ernst
Journal:  Neurochem Res       Date:  2013-09-26       Impact factor: 3.996

Review 3.  A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model.

Authors:  Terry Clayton; Michael M Poe; Sundari Rallapalli; Poonam Biawat; Miroslav M Savić; James K Rowlett; George Gallos; Charles W Emala; Catherine C Kaczorowski; Douglas C Stafford; Leggy A Arnold; James M Cook
Journal:  Int J Med Chem       Date:  2015-11-10

4.  Preparation of 6/8/11-Amino/Chloro-Oxoisoaporphine and Group-10 Metal Complexes and Evaluation of Their in Vitro and in Vivo Antitumor Activity.

Authors:  Qi-Pin Qin; Jiao-Lan Qin; Ting Meng; Gui-Ai Yang; Zu-Zhuang Wei; Yan-Cheng Liu; Hong Liang; Zhen-Feng Chen
Journal:  Sci Rep       Date:  2016-11-29       Impact factor: 4.379

5.  Towards functional selectivity for α6β3γ2 GABAA receptors: a series of novel pyrazoloquinolinones.

Authors:  Marco Treven; David C B Siebert; Raphael Holzinger; Konstantina Bampali; Jure Fabjan; Zdravko Varagic; Laurin Wimmer; Friederike Steudle; Petra Scholze; Michael Schnürch; Marko D Mihovilovic; Margot Ernst
Journal:  Br J Pharmacol       Date:  2017-12-22       Impact factor: 9.473

6.  Identification of novel positive allosteric modulators and null modulators at the GABAA receptor α+β- interface.

Authors:  Zdravko Varagic; Laurin Wimmer; Michael Schnürch; Marko D Mihovilovic; Shengming Huang; Sundari Rallapalli; James M Cook; Pantea Mirheydari; Gerhard F Ecker; Werner Sieghart; Margot Ernst
Journal:  Br J Pharmacol       Date:  2013-05       Impact factor: 8.739

7.  Design and Synthesis of Novel Deuterated Ligands Functionally Selective for the γ-Aminobutyric Acid Type A Receptor (GABAAR) α6 Subtype with Improved Metabolic Stability and Enhanced Bioavailability.

Authors:  Daniel E Knutson; Revathi Kodali; Branka Divović; Marco Treven; Michael R Stephen; Nicolas M Zahn; Vladimir Dobričić; Alec T Huber; Matheus A Meirelles; Ranjit S Verma; Laurin Wimmer; Christopher Witzigmann; Leggy A Arnold; Lih-Chu Chiou; Margot Ernst; Marko D Mihovilovic; Miroslav M Savić; Werner Sieghart; James M Cook
Journal:  J Med Chem       Date:  2018-03-06       Impact factor: 8.039

8.  Molecular tools for GABAA receptors: High affinity ligands for β1-containing subtypes.

Authors:  Xenia Simeone; David C B Siebert; Konstantina Bampali; Zdravko Varagic; Marco Treven; Sabah Rehman; Jakob Pyszkowski; Raphael Holzinger; Friederike Steudle; Petra Scholze; Marko D Mihovilovic; Michael Schnürch; Margot Ernst
Journal:  Sci Rep       Date:  2017-07-18       Impact factor: 4.379

  8 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.