115129-82-3Relevant academic research and scientific papers
Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: Synthesis, pharmacological evaluation, and cross-target QSAR studies
Lim, Herman D.,Istyastono, Enade P.,van de Stolpe, Andrea,Romeo, Giuseppe,Gobbi, Silvia,Schepers, Marjo,Lahaye, Roger,Menge, Wiro M.B.P.,Zuiderveld, Obbe P.,Jongejan, Aldo,Smits, Rogier A.,Bakker, Remko A.,Haaksma, Eric E.J.,Leurs, Rob,de Esch, Iwan J.P.
experimental part, p. 3987 - 3994 (2009/10/02)
Previous studies have demonstrated that clobenpropit (N-(4-chlorobenzyl)-S-[3-(4(5)-imidazolyl)propyl]isothiourea) binds to both the human histamine H3 receptor (H3R) and H4 receptor (H4R). In this paper, we describe the synthesis and pharmacological characterization of a series of clobenpropit analogs, which vary in the functional group adjacent to the isothiourea moiety in order to study structural requirements for H3R and H4R ligands. The compounds show moderate to high affinity for both the human H3R and H4R. Furthermore, the changes in the functional group attached to the isothiourea moiety modulate the intrinsic activity of the ligands at the H4R, ranging from neutral antagonism to full agonism. QSAR models have been generated in order to explain the H3R and H4R affinities.
N-(W-substituted alkyl)-'-(imidazol-4-yl)alkyl)guanidine
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, (2008/06/13)
N-(2-substituted alkyl)-N'[(imidazole-4-yl)alkylguanidines are provided by the reaction of a primary amine with benzoylisothiocyante to a benzoylthiourea derivative, followed by hydrolysis of this derivative to form the corresponding thiourea, converting this thiourea with methyliodide into an isothiourea and producing the desired compound by reaction of the isothiourea with aminopropylimidazole or aminoethylimidazole. The compound can be converted into an acid addition salt or the free compound obtained from such salt. The compounds are useful as the active ingredient in pharmaceutical compositions for the treatment of congestion, heart failure and some allergic conditions.
