Three (-)-cytisine derivatives and 1-hydroxyquinopimaric acid as acetylcholinesterase inhibitors.

ABSTRACT: In vitro acetylcholinesterase (AChE) inhibition was studied using novel derivatives of (-)-cytisine derivatives N-allylcytisine-12-carbamide (A-63), cytisine-12-carbamide (A-36), N-1-adamantylcytisine-12-thiocarbamide (U-12), and 1-hydroxyquinopimaric acid (U-201). Inhibition of acetylcholinesterase with compound A-63 was described as mixed inhibition. Substances (A-36) and (U-201) acted as competitive inhibitors with Ki equal to 6.71 mM and 3.89 mM, respectively, while (U-12) behaved as an uncompetitive inhibitor with Ki at 0.07 mM. The IC50 values were estimated at 1.47, 13.73, 3.39, and 7.81 mM, respectively. According to toxicity assessment, compound A-63 was non-toxic; it did not affect A. salina viability at a concentration less than 1000 ppm, while at 1000 ppm, only 3% mortality was

SUBMITTER: Garcia-Gracia JD 

PROVIDER: S-EPMC6718946 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature