the way to produce new labour union blokujacych h $2 histamine receptors

摘要

Heterocyclic cpds. of formula (I) and their salts are new: In (I) X3 and X2 are S, CHNO2 or NY, Y is H, OH, lower alkyl, CN or CONH2. R3 and R4 are each gps. of formula Het(CH2)mZ-(CH2)n, Het is (a) 2- or 4-imidazolyl opt. substd. by lower alkyl, halogen, CF3 or CH2OH (b) -2pyridyl opt. substd. by lower alkyl, halogen, NH2, OH or lower alkoxy, (c) 2-thiazolyl or 3-isothioazolyl, opt. substd. by Br, or (d) thiadizolyl opt. substd. by Cl or NH2, Z is S or CH2, m = 0-2, n = 2 or 3, m+n = 3 or 4, but can be 2 when the adjacent X3 or X4 gp. is S, CHNO2 or NCN. W is NH, or can be S when X3=X4=NH. p = 9-12. Cpds. (I) are histamine H2 receptor blockers. They inhibit histamine-induced gastric secretion, vasolidation and tachycardia. A typical cpd. is 1, 10-bis(N'-(2-(5-methyl-4-imidazolylmethylthio)ethyl)-guanidino)de- cane. In an example, this is prepd. from S-methyl-N-(2-(5-methyl-4-imidazolylmethylthio)ethyl)isothiouroni- um iodide and 1,10-diaminodecane.