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Synthesis and evaluation of potential biologically active rhodanine derivatives and analogues
Šimková, Adéla ; Krátký, Martin (advisor) ; Matouš, Petr (referee)
The topic of this thesis is the synthesis of rhodanine derivatives and evaluation of their biological activity, particularly as potential cholinesterases inhibitors. This group of compounds is important for treatment of many diseases, e.g., Alzheimer's disease or myasthenia gravis. All synthetized compounds are based on structure of rhodanine (2-thioxothiazolidine- 4-one), which is an important heterocyclic compound with a wide spectrum of biological properties. Its structure can be modified in many ways, which can be used in the development of new drugs. Its derivatives have been shown to have, for example, anti-inflammatory, anticancer, antibacterial and antifungal activities, as well as inhibitory activity against several enzymes, e.g., cholinesterases. Seventeen compounds were synthesized in sufficient amount for characterisation and assessment of biological activity (7-93 %). Most of them are amides based on the structure of 2-thioxothiazolidine-4-one and thiazolidine-2,4-dione, that were prepared by carbodiimide- mediated coupling, other derivatives are based on the structure of 2-thioxothiazolidine-4-one and from 2,4-dioxothiazolidine-3-acetic acid. These compounds were prepared by Knoevenagel condensation in glacial acetic acid. All compounds were tested for their inhibitory activity...
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Synthesis and evaluation of potential biologically active rhodanine derivatives and analogues
Šimková, Adéla ; Krátký, Martin (advisor) ; Matouš, Petr (referee)
The topic of this thesis is the synthesis of rhodanine derivatives and evaluation of their biological activity, particularly as potential cholinesterases inhibitors. This group of compounds is important for treatment of many diseases, e.g., Alzheimer's disease or myasthenia gravis. All synthetized compounds are based on structure of rhodanine (2-thioxothiazolidine- 4-one), which is an important heterocyclic compound with a wide spectrum of biological properties. Its structure can be modified in many ways, which can be used in the development of new drugs. Its derivatives have been shown to have, for example, anti-inflammatory, anticancer, antibacterial and antifungal activities, as well as inhibitory activity against several enzymes, e.g., cholinesterases. Seventeen compounds were synthesized in sufficient amount for characterisation and assessment of biological activity (7-93 %). Most of them are amides based on the structure of 2-thioxothiazolidine-4-one and thiazolidine-2,4-dione, that were prepared by carbodiimide- mediated coupling, other derivatives are based on the structure of 2-thioxothiazolidine-4-one and from 2,4-dioxothiazolidine-3-acetic acid. These compounds were prepared by Knoevenagel condensation in glacial acetic acid. All compounds were tested for their inhibitory activity...
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