1822-49-7Relevant academic research and scientific papers
Synthesis of Isothiourea Derivatives
Horiuchi, Jiro,Suzuki, Kazuo,Shitara, Eiki,Niwa, Ryuji,Kato, Tetsuzo
, p. 1080 - 1084 (2007/10/02)
The reaction of thioureas (9) with 2-chloromethylpyridine hydrochloride (5), 3-chloromethylpyridine hydrochloride (6), 2-chloromethylquinoline hydrochloride (7), and 5-chloromethyl-4-methylimidazole hydrochloride (8) gave the isothiourea dihydrochlorides
Synthesis and Antisecretory and Antiulcer Activities of Derivatives and Analogues of 2-(2-Pyridyl)tetrahydrothiophene-2-carbothioamide
Aloup, Jean-Claude,Bouchaudon, Jean,Farge, Daniel,James, Claude,Deregnaucourt, Jean,Hardy-Houis, Monique
, p. 24 - 29 (2007/10/02)
New thioamide derivatives of 2-(2-pyridyl)tetrahydrothiophene-2-carbothioamide (29) and related compounds (in which the tetrahydrothiophene ring was replaced by tetrahydrothiopyran, tetrahydrofuran, 1,3-dithiane, or 1,3-oxathiane and where the pyridine ring was repleaced by other nitrogen heterocycles) were synthesized and tested for their antisecretory and antiulcer activities.These thioamides were prepared according to one of the following methods: (i) reaction of an isothiocyanate with the carbanion of the corresponding cyclic precursor (for secondary thioamides); (ii) reaction of ammonia or an amine with the dithio ester prepared from the same precursor (for primary, secondary, and tertiary thioamides).These thioamides were evaluated by the Shay method to measure their antisecretory activity and by the stress-induced-ulcer method to test their antiulcer activity.Structure-activity relationships are discussed.N-Methyl-2-(2-pyridyl)tetrahydrothiophene-2-carbothioamide (R.P. 40749,30) exhibited activities that were at least 10 times higher than those reported for cimetidine.
2-(Pyrid-2-yl)tetrahydrothiophene derivatives
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, (2008/06/13)
Compounds of the formula: STR1 wherein R represents hydrogen or alkyl of 1 through 4 carbon atoms, and R1 and R2 represent hydrogen or alkyl of 1 through 15 carbon atoms, or alkyl of 1 through 15 carbon atoms substituted by one substituent selected from (i) hydroxy, (ii) alkylamino in which the alkyl radical is of 1 through 4 carbon atoms, (iii) dialkylamino in which the alkyl radicals are of 1 through 4 carbon atoms, (iv) phenyl, (v) carboxy, and (vi) alkoxycarbonyl in which the alkoxy radical is of 1 through 4 carbon atoms, or R1 and R2 together with the nitrogen atom to which they are attached represent a five- or six-membered heterocyclic radical, are new compounds. They possess pharmacological properties and are particularly useful in the treatment of gastro-intestinal ulcers.
