Synthesis and anticonvulsant properties of 1,2,3,4-tetrahydroisoquinolin-1-ones

Abstract

Following our previous molecular modeling studies we herein report the synthesis of substituted 1,2,3,4-tetrahydroisoquinolinone-4-carboxylic acids in an attempt to obtain new anticonvulsants acting as negative modulators of AMPA-type glutamate receptor. The evaluation of their pharmacological effects demonstrated that some derivatives were able to prevent audiogenic induced seizures in DBA/2 mice.

Heterogeneous Catalytic Method for the One-pot Three-component Synthesis of Isoquinolonic Acid Derivatives Catalyzed by a 4Å Molecular Sieves Supported Lanthanum Catalyst

“…Tetrahydroisoquinolonic acids form an important class of heterocyclic compounds since they possess exhibit several pharmaceutical and biological activities. These compounds have been demonstrated to act as anticancer [1,2], anticonvulsant [3,4] and antidiabetic agents [5]. Furthermore, they are known have served as starting material for the total synthesis of natural products, such as the benzophenanthridine alkaloids nitidine chloride [6] and (±)-corynoline [7], as well as the 3-arylisoquinoline alkaloid decumbenine B [8].…”

Novel 1H-2-Benzopyran-1-One and 2,3-Benzodiazepin-1-One Derivatives

“…1H-2-Benzopyran-1-ones (isocoumarins) and their 3,4dihydro derivatives are a class of natural products that occur as microbial metabolites and exhibit interesting biological properties. [1][2][3][4][5][6][7][8][9][10][11][12] The authors' objective was to construct the desired isocoumarin derivatives and study their behaviour towards different nucleophilic reagents.…”