| Title : Synthesis and preliminary biological evaluations of (+)-isocampholenic acid-derived amides - Groselj_2016_Mol.Divers_20_667 |
| Author(s) : Groselj U , Golobic A , Knez D , Hrast M , Gobec S , Ricko S , Svete J |
| Ref : Mol Divers , 20 :667 , 2016 |
|
Abstract :
The synthesis of two novel (+)-isocampholenic acid-derived amines has been realized starting from commercially available (1S)-(+)-10-camphorsulfonic acid. The novel amines as well as (+)-isocampholenic acid have been used as building blocks in the construction of a library of amides using various aliphatic, aromatic, and amino acid-derived coupling partners using BPC and CDI as activating agents. Amide derivatives have been assayed against several enzymes that hold potential for the development of new drugs to battle bacterial infections and Alzheimer's disease. Compounds 20c and 20e showed promising selective sub-micromolar inhibition of human butyrylcholinesterase. HBChE IC50 0.80 +/- 0.05 and 0.25 +/- 0.02 microM respectively. |
| PubMedSearch : Groselj_2016_Mol.Divers_20_667 |
| PubMedID: 27017352 |
Groselj U, Golobic A, Knez D, Hrast M, Gobec S, Ricko S, Svete J (2016)
Synthesis and preliminary biological evaluations of (+)-isocampholenic acid-derived amides
Mol Divers
20 :667
Groselj U, Golobic A, Knez D, Hrast M, Gobec S, Ricko S, Svete J (2016)
Mol Divers
20 :667