[2-Amino-2-thiazoline derivatives--a novel chemotype possessing muscarinomimetic effect].

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 (EC50 = 13 +/- 2 microM).

[The pharmacological selectivity of cholinesterase inhibitors is due to their antagonism with calcium ions].

The inhibitory activity of O-carbamoyl acylhydroxymoylchlorides was studied on the purified specimens of acetylcholinesterase from human erythrocytes and butirylcholinesterase from the horse blood serum. The pharmacological activity of these compounds was studied on isolated organs of rats. It was shown that introduction of N-aryl substituent in carbamate molecule increases the anticholinesterase activity and efficacy of blocking the neuromuscular conductivity.