Non-imidazole histamine H 3 ligands: part V. synthesis and preliminary pharmacological investigation of 1-[2-thiazol-4-yl- and 1-[2-thiazol-5-yl-(2-aminoethyl)]-4- n -propylpiperazine derivatives

Series of 1-[2-thiazol-4-yl-(2-aminoethyl)]- and 1-[2-thiazol-5-yl-(2-aminoethyl)]-4- -propylpiperazine derivatives have been prepared and in vitro tested as H -receptor antagonists (the electrically evoked contraction of the guinea-pig jejunum). It appeared that by comparison of homologous pairs, t...

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Bibliographic Details
Published in:Medicinal chemistry research 2013-08, Vol.22 (8), p.3640
Main Authors: Guryn, Roman, Staszewski, Marek, Walczyński, Krzysztof
Format: Article
Language:English
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Summary:Series of 1-[2-thiazol-4-yl-(2-aminoethyl)]- and 1-[2-thiazol-5-yl-(2-aminoethyl)]-4- -propylpiperazine derivatives have been prepared and in vitro tested as H -receptor antagonists (the electrically evoked contraction of the guinea-pig jejunum). It appeared that by comparison of homologous pairs, the 1-[2-thiazol-5-yl-(2-aminoethyl)]-4- -propylpiperazines ( , and - ) have much higher potency than their analogous 1-[2-thiazol-4-yl-(2-aminoethyl)]-4- -propylpiperazines ( - ). Based on the obtained results, we observed the 5-position of 2-methyl-2-R-aminoethyl substituents in the thiazole ring is favourable for histamine H receptor antagonist activity, whereas its presence in position 4 leads, almost in each case, to strong decrease of activity.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-012-0372-8