89980-86-9Relevant academic research and scientific papers
A guanidinium ion-based anion- and solvent polarity-controllable molecular switch
Lin, Tzu-Chiun,Lai, Chien-Chen,Chiu, Sheng-Hsien
supporting information; experimental part, p. 613 - 616 (2009/09/27)
(Chemical Equation Presented) The macrocycle bis-p-xylyl[26]crown-6 (BPX26C6) is capable of complexing guanidinium ions in a [2]pseudorotaxane-like manner in solution. A corresponding molecular switch can be operated through changes in solvent polarity or the addition and removal of halogen and acetate anions.
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.
