Literature DB >> 16677814

Synthesis and SAR of novel histamine H3 receptor antagonists.

Cynthia D Jesudason1, Lisa S Beavers, Jeffrey W Cramer, Joelle Dill, Don R Finley, Craig W Lindsley, F Craig Stevens, Robert A Gadski, Samuel W Oldham, R Todd Pickard, Christopher S Siedem, Dana K Sindelar, Ajay Singh, Brian M Watson, Philip A Hipskind.   

Abstract

The synthesis and biological evaluation of novel tetrahydroisoquinoline, tetrahydroquinoline, and tetrahydroazepine antagonists of the human and rat H(3) receptors are described. The substitution around these rings as well as the nature of the substituent on nitrogen is explored. Several compounds with high affinity and selectivity for the human and rat H(3) receptors are reported.

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Year:  2006        PMID： 16677814     DOI： 10.1016/j.bmcl.2006.04.004

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


  4 in total

1.  Synthesis of a unique isoindoline/tetrahydroisoquinoline-based tricyclic sultam library utilizing a Heck-aza-Michael strategy.

Authors:  Qin Zang; Salim Javed; Patrick Porubsky; Farman Ullah; Benjamin Neuenswander; Gerald H Lushington; Fatima Z Basha; Michael G Organ; Paul R Hanson
Journal:  ACS Comb Sci       Date:  2012-02-06       Impact factor: 3.784

2.  A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin.

Authors:  J Phillip Kennedy; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2009-05-03       Impact factor: 2.823

3.  Comparison of Different 2D and 3D-QSAR Methods on Activity Prediction of Histamine H3 Receptor Antagonists.

Authors:  Siavoush Dastmalchi; Maryam Hamzeh-Mivehroud; Karim Asadpour-Zeynali
Journal:  Iran J Pharm Res       Date:  2012       Impact factor: 1.696

4.  A robust iron catalyst for the selective hydrogenation of substituted (iso)quinolones.

Authors:  Basudev Sahoo; Carsten Kreyenschulte; Giovanni Agostini; Henrik Lund; Stephan Bachmann; Michelangelo Scalone; Kathrin Junge; Matthias Beller
Journal:  Chem Sci       Date:  2018-09-06       Impact factor: 9.825
  4 in total

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