127785-95-9Relevant academic research and scientific papers
Design, synthesis, and pharmacological evaluation of conformationally constrained analogues of N,N'-diaryl- and N-aryl-N-aralkylguanidines as potent inhibitors of neuronal Na+ channels
Maillard, Michel C.,Perlman, Michael E.,Amitay, Oved,Baxter, Deborah,Berlove, David,Connaughton, Sonia,Fischer, James B.,Guo, Jun Qing,Hu, Lain-Yen,McBurney, Robert N.,Nagy, Peter I.,Subbarao, Katragadda,Yost, Elizabeth A.,Zhang, Lu,Durant, Graham J.
, p. 3048 - 3061 (2007/10/03)
In the present investigation, the rationale for the design, synthesis, and biological evaluation of potent inhibitors of neuronal Na+ channels is described. N,N'-Diaryl- and N-aryl-Naralkylguanidine templates were locked in conformations mimick
New tetracyclic guanidine derivatives with H1-antihistaminic properties. Chemistry of epinastine
Walther,Daniel,Bechtel,Brandt
, p. 440 - 446 (2007/10/02)
A series of new tetracyclic guanides were synthesized by various methods. Specific binding of the described compounds to histamine-1 and histamine-2 receptors was determined. The compound 3-amino-9, 13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine (epinastine, WAL 801) combines high selectivity with high affinity for the H1 receptor and was selected from the compounds studied for further pharmacological and clinical investigations. Experimentally determined physicochemical parameters (pk(a)-value, partition coefficient) and the hydrogen-bonding ability of epinastine are indications that this compound will not easily cross the blood-brain barrier. This explains the absence of CNS side-effects of epinastine in pharmacological and clinical studies.
