Derivatives of 2-amino-2-thiazoline - novel chemotype with muscarinomimetic activity


1. Institute of Physiologically Active Compounds Russ. Acad. Sci. Russia
Type: Experimental/clinical study
PubMed Id: 14569878
Year: 2003 vol: 49  issue:1  pages: 92-95
Abstract: Derivatives of 2-amino-2-thiazoline exhibit muscarinomimetic properties in model experiments with isolated rat ileum. The activity of compounds strongly depends on the nature of substituents in 5-position of thiazoline ring. The most active spasmogenic compound is 5-iodomethyl-2-amino-2-thiazoline hydroiodide (ЕС50 =13±2 mМ). Its effect is very similar to activity of cholinergic agent pilocarpine (ЕС50 =14±4 mМ), but "intrinsic activity" parameter a (a=0.87±0.12) of 5-iodomethyl-2-amino-2-thiazoline was more significant. Ileum contractions induced by this compounds were inhibited by atropine. Derivatives of 2-amino-2-thiazoline (like pilocarpine) were not demonstrated nicotinomimetic properties. These compounds demonstrate very weak anti-AChE activity. For 5-iodomethyl-2-amino-2-thiazoline hydroiodide the IС50 value is 0.39±0.09 mM.
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Reference: Ivanov Yu.Ya., Tkachenko S.E., Proshin A.N., Bachurin S.O., Derivatives of 2-amino-2-thiazoline - novel chemotype with muscarinomimetic activity, Biomeditsinskaya khimiya, 2003, vol: 49(1), 92-95.