18371-53-4Relevant academic research and scientific papers
A convenient one-pot three component approach to synthesis of highly substituted iminothiazolines
Samimi, Heshmat Allah,Mamaghani, Manouchehr,Tabatabaeian, Khalil
experimental part, p. 2825 - 2833 (2011/04/17)
An efficient one-pot three component method was developed for the synthesis of highly substituted 2-iminothizolines by the reaction of isothiocyanates, primary amines and α-bromoketones in ambient temperature. The reaction produced the desired products in a completely regioselective manner in excellent yields (78-94%). The Japan Institute of Heterocyclic Chemistry.
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.
