Novel Anticholinesterase Carbamates
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Novel Anticholinesterase Carbamates
This invention relates to synthesis of new biologically active chemical compounds.
More particularly, the invention relates to molecular design of novel carbamate esters, which are strong cholinesterase (ChE) inhibitors.
The invention is concerned with original carbamate esters of α-amino oximes (basic chain structure [ I ]).
The compounds containing chain [I] incorporated into suitable molecular skeleton are potent inhibitors of ChE-type enzymes, respecting the nature of ester function and structural analogy to natural substrate in some important details.
The presented work describes constitution, structural stability factors, syntheses and basic anti-ChE activity of some representative compounds.
- These compounds posses utility in all fields where are required strong and selective ChE inhibitors, i.e., in the fields of pesticides and pharmaceuticals.
- Extremely high affinity of some derived compounds to both type of ChE enzymes (serum- or pseudo- and true ChE) are in accordance with experimentally confirmed low toxicity for mammals (protected by serum-ChE in peripheral bloodstream) and high toxicity for insects (without mentioned protection).
- A variation, structurally related to quinine moiety, exhibit strongly lipophylic character and resistancy to peripheral pseudo-ChE. That indicates to CNS targeted activity with possible use in treatment of health problems positively responding to ChE suppression in CNS, for example in case of Myasthenia gravis and Alzheimer’s disease. Because of possibilities for structural optimization, from that type of compounds may result more acceptable anti-ChE drug than relatively invariable physostig mine and similar compounds.
- The presented basic structure opens numerous courses of development, and current results are not conclusive
