Literature DB >> 10386938

Structure-activity relationships of substituted 5H-thiazolo[3,2-a]pyrimidines as group 2 metabotropic glutamate receptor antagonists.

J Wichmann1, G Adam, S Kolczewski, V Mutel, T Woltering.   

Abstract

A series of 5H-thiazolo[3,2-a]pyrimidine derivatives 1 was studied with respect to the inhibition of 1S,3R-ACPD (10 microM)-stimulated GTP gamma35S binding on rat mGlu2 receptor transfected cell membranes. The influence of substituents at position 6 and 7 as well as the substitution pattern of the two phenyl-rings in position 2 and 5 on the activity is discussed.

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Year:  1999        PMID： 10386938     DOI： 10.1016/s0960-894x(99)00227-9

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

Review 1.  Recent progress in the synthesis and characterization of group II metabotropic glutamate receptor allosteric modulators.

Authors:  Douglas J Sheffler; Anthony B Pinkerton; Russell Dahl; Athina Markou; Nicholas D P Cosford
Journal:  ACS Chem Neurosci       Date:  2011-04-12       Impact factor: 4.418

Review 2.  Recent progress in asymmetric Biginelli reaction.

Authors:  Majid M Heravi; Shima Asadi; Boshra Malekzadeh Lashkariani
Journal:  Mol Divers       Date:  2013-04-16       Impact factor: 2.943

3.  Ethyl (2Z)-2-(3-methoxy-benzyl-idene)-7-methyl-3-oxo-5-phenyl-2,3-dihydro-5H-1,3-thia-zolo[3,2-a]pyrimidine-6-carboxyl-ate.

Authors:  Mukesh M Jotani; Bharat B Baldaniya; Jerry P Jasinski
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-02-13

4.  (Z)-Ethyl 2-(2,4-dimethyl-benzyl-idene)-7-methyl-3-oxo-5-phenyl-3,5-dihydro-2H-thia-zolo[3,2-a]pyrimidine-6-carboxyl-ate.

Authors:  Xiao-Yan Chen; Han-Chu Wang; Qian Zhang; Zhi-Jian Song; Fei-Yun Zheng
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-12-14

5.  Ethyl (Z)-2-(2-fluoro-benzyl-idene)-7-methyl-3-oxo-5-phenyl-3,5-dihydro-2H-thia-zolo[3,2-a]pyrimidine-6-carboxyl-ate.

Authors:  Cheng-Guang Zhao; Jie Hu; Ya-Li Zhang; Jing Zhang; Shu-Lin Yang
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-10-22

6.  Synthesis, Antibacterial and Antitubercular Activities of Some 5H-Thiazolo[3,2-a]pyrimidin-5-ones and Sulfonic Acid Derivatives.

Authors:  Dong Cai; Zhi-Hua Zhang; Yu Chen; Xin-Jia Yan; Liang-Jing Zou; Ya-Xin Wang; Xue-Qi Liu
Journal:  Molecules       Date:  2015-09-10       Impact factor: 4.411

7.  Allosteric modulators for mGlu receptors.

Authors:  F Gasparini; W Spooren
Journal:  Curr Neuropharmacol       Date:  2007-09       Impact factor: 7.363

8.  Herbicidal properties of antihypertensive drugs: calcium channel blockers.

Authors:  Hannan Safiyyah Tan Sian Hui Abdullah; Poh Wai Chia; Dzolkhifli Omar; Tse Seng Chuah
Journal:  Sci Rep       Date:  2021-07-09       Impact factor: 4.379

9.  Synthesis and Cytotoxic Activity of New Thiazolopyrimidine Sugar Hydrazones and Their Derived Acyclic Nucleoside Analogues.

Authors:  Ebtesam A Basiony; Allam A Hassan; Zahra M Al-Amshany; Ahmed A Abd-Rabou; Adel A-H Abdel-Rahman; Nasser A Hassan; Wael A El-Sayed
Journal:  Molecules       Date:  2020-01-18       Impact factor: 4.411
  9 in total

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