Synthesis of pyridyl isosteres of thioperamide as H3-receptor histamine antagonists

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Title:Synthesis of pyridyl isosteres of thioperamide as H3-receptor histamine antagonists
Creators:
Ganellin, C. Robin
Jayes, Dalia
Khalaf, Yasmin S.
Tertiuk, Wasyl
Arrang, Jean-Michel
Defontaine, Nadia
Schwartz, Jean-Charles
Journal or Publication Title:
Collection of Czechoslovak Chemical Communications, 56, 11, pp. 2448-2455

Abstract

The synthesis and evaluation as H<sub>3</sub>-receptor histamine antagonists is described of novel isoteric analogues of thioperamide. The compounds are designed to have fewer NH groups in order to assist brain penetration. However none of the compounds is sufficiently active as an antagonist in vitro. The 2-pyridyl analogue <i>II</i> has <i>K</i><sub>i</sub> = 13 μmol 1<sup>-1</sup>.

Title:Synthesis of pyridyl isosteres of thioperamide as H3-receptor histamine antagonists
Creators:
Ganellin, C. Robin
Jayes, Dalia
Khalaf, Yasmin S.
Tertiuk, Wasyl
Arrang, Jean-Michel
Defontaine, Nadia
Schwartz, Jean-Charles
Divisions:Life and Chemical Sciences > Institute of Organic Chemistry and Biochemistry > Collection of Czechoslovak Chemical Communications
Journal or Publication Title:Collection of Czechoslovak Chemical Communications
Volume:56
Number:11
Page Range:pp. 2448-2455
ISSN:0010-0765
E-ISSN:1212-6950
Publisher:Institute of Organic Chemistry and Biochemistry
Related URLs:
URLURL Type
http://dx.doi.org/10.1135/cccc19912448UNSPECIFIED
ID Code:5176
Item Type:Article
Deposited On:22 Feb 2010 11:32
Last Modified:22 Feb 2010 10:32

Citation

Ganellin, C. Robin; Jayes, Dalia; Khalaf, Yasmin S.; Tertiuk, Wasyl; Arrang, Jean-Michel; Defontaine, Nadia; Schwartz, Jean-Charles (1991) Synthesis of pyridyl isosteres of thioperamide as H3-receptor histamine antagonists. Collection of Czechoslovak Chemical Communications, 56 (11). pp. 2448-2455. ISSN 0010-0765

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