Synthesis and biological activity of substituted 7-aza-8-aza(oxa)-bicyclo[4.3.0]-6,9-nonadienes

Synthesis, anticonvulsant activity and <i>in silico</i> study of some novel amino acids incorporated bicyclo compounds

“…Hence, with all of these factors in mind, it has been suggested that the focus of epilepsy research should be directed to identifying the underlying mechanism of epileptogenesis and the subsequent "expression" of seizure activity, rather than resorting primarily to symptom control, that is, mere suppression of seizures (McNamara, 2001). The analogues of bicyclic systems, 8, 10-diza-bicyclo [4.3.1] decane and 3, 10-diza-bicyclo [4.3.1] decane bicyclo compounds, have been found to possess a wide range of biological activities, which include analgesic, anti inflammatory (Peter 2008, Nagaev et al, 1999, Pinna et al, 2000, muscarinic receptor antagonist (Myoung et al, 2003), antibacterial (Smirnova et al, 1995), antiviral (Miller et al, 2001), antiprotozoal (Seeacher et al, 2005) and antispasmolytic (Rajdan et al, 1987) but still no one has reported/studied, such compounds as anticonvulsants. The reason to incorporate biologically friendly amino acids into pharmacologically active moiety is not only to minimize the side effects of the metabolites of the parent compound upon metabolism in the body but also to direct the drug for specific site and in order to enhance the hydrophilicity of the synthesized candidates, like bicyclo compounds may exhibit potent anticonvulsant activity.…”

The Reaction of 5-Amino-3-(cyanomethyl)-1H-pyrazol-4-carbonitrile with beta-Cycloketols

“…However, the heterocyclization reactions of β-cycloketols are not well studied. Thus, the literature describes the preparation of isoquinolines 2 [3][4][5][6][7], indazoles 3 [8][9][10], benzo[c]isoxazoles 4 [9,10], [1,2,4]triazolo [3-b]quinazolines 5 [11] and pyrazolo[3-c]isoquinolines 6 [12] (Scheme 1) by reactions of beta-cycloketols with various 1,2-and 1,3-dinucleophilic agents. Despite the large attention paid to reactions of aminoazoles with 1,3-dielectrophilic agents (see reviews [13,14]), only a few examples of reactions involving β-cycloketols were found in the literature.…”