145012-90-4Relevant academic research and scientific papers
A Mild and Efficient Method for the Preparation of Guanidines
Poss, Michael A.,Iwanowicz, Edwin,Reid, Joyce A.,Lin, James,Gu, Zhengxiang
, p. 5933 - 5936 (1992)
A mild and efficient method for the preparation of guanidines by reaction of an acylated thiourea with an amine followed by removal of the acyl groups(s) from the intermediate acylguanidine is reported.Key Words: acylguanidine, acylthiourea, guanidine, water soluble carbodiimide
Isothiourea analogues of histamine as potent agonists or antagonists of the histamine H3-receptor
Van der Goot,Schepers,Sterk,Timmerman
, p. 511 - 517 (2007/10/02)
The synthesis and H3-activity of a series of isothiourea analogues of histamine have been described. It has been shown that S-[2-(4(5)-imidazolyl)ethylisothiourea (VUF 8325) is a potent H3-agonist measured as the electrically evoked contraction of the guinea-pig ileum. Upon methylation of the imidazole system or the isothiourea moiety a decrease in affinity was observed leading to either weak agonists or weak antagonists. Introduction of N-(phenylalkyl) substituents at the isothiourea part gives rise to highly potent H3-antagonists. Particularly the 4-chlorobenzyl group appeared to be favourable in the series described resulting in a histamine H3-antagonist with a pA2-value of 9.9.
