64801-78-1Relevant articles and documents
Synthesis and biological assays of new H3-antagonists with imidazole and imidazoline polar groups
Mor, Marco,Bordi, Fabrizio,Silva, Claudia,Rivara, Silvia,Zuliani, Valentina,Vacondio, Federica,Morini, Giovanni,Barocelli, Elisabetta,Ballabeni, Vigilio,Impicciatore, Mariannina,Plazzi, Pier Vincenzo
, p. 27 - 34 (2000)
New histamine H3-receptor antagonists were synthesised and tested on rat brain membranes and on electrically stimulated guinea-pig ileum. The new compounds have a central polar group represented by a 2-alkylimidazole or a 2-thioimidazoline nucleus. The effect of the polar group basicity on the optimal length of the alkyl chain, connecting this group to a 4(5)-imidazolyl ring, was investigated. The best affinity values, obtained by displacement of [3H]-RAMHA from rat brain, were obtained for the 2-alkylimidazole derivatives (2a-f) with tetramethylene chain (pK(i) 8.03-8.97), having an intermediate basicity between that of the previously reported 2- thioimidazoles (1a-i) and that of 2-alkylthioimidazolines (3a-h). In contrast, a general lowering of affinity (pK(i) 5.90-7.63) was observed for compounds of the last series (3a-h), with a complex dependence on the terminal lipophilic group and chain length. (C) 2000 Elsevier Science S.A.
IMIDAZOLINE DERIVATIVES AS CXCR4 MODULATORS
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Page/Page column 91; 93; 100-102, (2020/10/19)
The present invention provides novel compounds of formula (I) and pharmaceutical compositions containing these compounds. The compounds of formula (I) can act as CXCR4 modulators that specifically target the CXCR4 minor pocket, and they have further been
Method of making imidazole-2-thiones
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Page/Page column 3; 8-9, (2008/06/13)
The present invention provides a method of making an imidazole-2-thione which comprises the steps of reacting a vicinal diamine with a compound having a thiocarbonyl moiety and oxidizing the resulting reaction product to obtain said imidazole-2-thione.