Histamine H2-receptor agonists. Synthesis, in vitro pharmacology, and qualitative structure-activity relationships of substituted 4- and 5-(2-aminoethyl)thiazoles

1992 ◽  
Vol 35 (17) ◽  
pp. 3239-3246 ◽  
Author(s):  
John C. Eriks ◽  
Henk Van der Goot ◽  
Geert Jan Sterk ◽  
Hendrik Timmerman
Keyword(s):  
Histamine H2 Receptor ◽  
H2 Receptor ◽  
Structure Activity Relationships ◽  
Receptor Agonists ◽  
Structure Activity ◽  
In Vitro Pharmacology ◽  
Qualitative Structure

Structure-Activity Relationships of Histamine H2 Receptor Ligands+

2004 ◽  
Vol 4 (9) ◽  
pp. 941-954 ◽  
Author(s):  
Stefan Dove ◽  
Sigurd Elz ◽  
Roland Seifert ◽  
Armin Buschauer
Keyword(s):  
Receptor Ligands ◽  
Histamine H2 Receptor ◽  
H2 Receptor ◽  
Structure Activity Relationships ◽  
Structure Activity

scholarly journals Novel Azolylalkyloxy Compounds with Antipicornaviral Activity

1995 ◽  
Vol 6 (4) ◽  
pp. 245-254 ◽  
Author(s):  
M. D. Abel ◽  
A. D. Cameron ◽  
C. M. Ha ◽  
C. A. Koski ◽  
H. T. Luu ◽  
...  
Keyword(s):  
Vitro Activity ◽  
In Vitro Activity ◽  
Optimal Length ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Wide Range ◽  
Highly Effective ◽  
Qualitative Structure

A novel series of azolylalkyloxy compounds was designed, synthesized and evaluated for antipicornaviral activity. Several of the compounds exhibited in vitro activity comparable to that of Disoxarll. An investigation of qualitative structure-activity relationships indicated that the optimal length of the alkyI chain is six or seven carbon atoms, with seven being marginally superior. The effect of different azole moieties on activity was relatively small, with 3-methylisoxazole and 4-methylthiazole being most effective. The nature of the oxy substituent was found to be extremely important for antipicornaviral activity. The 2-dibenzofuryl group proved to be the most effective oxy substituent for this class of compounds. Compounds 11 and 22, combining dibenzofuran with 3-methylisoxazole and 4-methylthiazole, respectively, were highly effective in vitro against a wide range of human rhinoviruses as well as several enteroviruses.

Synthesis, in vitro pharmacology, and structure–activity relationships of 2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as mGluR2 antagonists

2006 ◽  
Vol 14 (10) ◽  
pp. 3405-3420 ◽  
Author(s):  
Akito Yasuhara ◽  
Kazunari Sakagami ◽  
Ryoko Yoshikawa ◽  
Shigeyuki Chaki ◽  
Masato Nakamura ◽  
...  
Keyword(s):  
Dicarboxylic Acid ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
In Vitro Pharmacology

Structure-activity relationship of histamine H2-receptor agonists

1978 ◽  
Vol 8 (4) ◽  
pp. 396-397
Author(s):  
H. -G. Lennartz ◽  
S. Schwarz ◽  
M. Hepp ◽  
W. Schunack
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Histamine H2 Receptor ◽  
H2 Receptor ◽  
Receptor Agonists ◽  
Structure Activity ◽  
Relationship Of
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